International Conference on Pharmaceutical Chemistry September 05-07, 2016 Frankfurt, Germany

Biography:

Wei Li has been on faculty at University of Tennessee Health Science Center, USA after obtaining his PhD in Chemistry from Columbia University in the City of New York in 1999. He is currently a Professor and the Faculty Director of Shared Analytical Instrument in the university. He has publised over 114 peer-reviewed papers and three book chapters, is an inventor of a number of issued patents, and serves as the Editor of the Anticancer Section of Current Medicinal Chemistry. He is a frequent grant reviewer for NIH and other funding agencies, and his current research is supported by multiple NIH grants

Abstract:

Malignant melanoma is the most aggressive form of skin cancer and it is highly resistant to most existing therapies. Despite recent advances in both targeted therapy (e.g. BRAF inhibitors vemurafenib and dabrafenib; MEK inhibitor trametinib) and immunotherapy (ipilimumab; pembrolizumab), acquired drug resistance often develops quickly and the overall survival for malignant melanoma remains unsatisfactory. Chemotherapeutic drugs including tubulin inhibitors (e.g., paclitaxel or vinblastine) are used in treating malignant melanoma clinically, but their efficacy is often limited by the ABC-transporter mediated drug efflux and non-specific tissue distribution, leading to dose limiting toxicity. We have discovered several sets of novel tubulin inhibitors that:  1) target the colchicine binding site in tubulin and have broad spectrum of potent anticancer activity; 2) effectively circumvent major drug resistance mechanisms (P-gp, BCRP, and MRPs) that hinder the clinical efficacy with existing tubulin inhibitors; 3) are orally bioavailable and have excellent drug-like properties; 4) are efficacious against both drug sensitive and drug resistant melanoma tumors in vivo; and 5) have strong synergy with approved BRAF inhibitors for BRAF-resistant melanoma tumors. We have also developed nanoparticle formulations for these agents and showed that these targeted drug delivery approaches can significantly improve the anticancer efficacy for these tubulin inhibitors. 

Biography:

Sylvia Wagner studied Chemistry at the University Karlsruhe. She did her PhD thesis at the Fraunhofer IBMT, where she is Group Manager of the Preclinical Nanotechnology & Nanotoxicology group since 2008 and Head of Department Bioprocessing & Bioanalytics since 2015. Her main research topics are focused on nanobiotechnology and development of in vitro/ex vivo models for preclinical testing of new nanoparticulate formulations and nanosafety issues. For example, formulations for the specific drug targeting (e.g., tumor targeting) as well as for crossing of biological barriers (e.g., blood-brain barrier or gastrointestinal barrier) are mainly on focus. 

Abstract:

Since many centuries there have been huge challanges in medicine. For example, evolution gave birth to an extremely useful structure: The blood-brain barrier (BBB) that protects our central nervous system homeostasis by shielding off toxic substances and pathogens. But biologically valuable does not always mean pharmacologically welcome. The BBB does not distinguish between friend and foe and causes many potentially effective brain therapeutics to fail in vivo - not because of a lack of potency, but because they cannot pass this barrier. This dilemma especially comes into focus for the rapidly growing numbers of neurodegenerative disorders. Another example comes from tumor therapy. The main disadvantages of conventional chemotherapy are modest tumor response and dose limiting side effects because of non-specific action of drugs to all fast proliferating tissues. Both described scenarios are still unsolved problems in modern medicine. However today, we can use the elegant approach of molecular Trojan Horses: the fast-emerging field of nanotechnology offers the possibility to enlarge the pool of substances by packing promising drugs into nanoparticles (NP). NP show a high drug loading efficiency with minor drug leakage as well as the ability to circumvent multi­drug resistance paired with good storage stability. By this, we can mask the original physicochemical properties of substances and even surface-modify the NP with ligands targeting specific receptors e.g. at the BBB or on cancer cells. The advantages are tempting: Apart from reducing peripheral doses and consequently side effects, drugs can be delivered directly to target structures. 

Biography:

Jun Fang has completed his PhD at Kumamoto University Medical School in 2003 and 2-year Post-doctoral studies from Duke University Medical Center. He is the Associate Professor of DDS Research Institute/Faculty of Pharmaceutical Science at Sojo University, Japan. His major research topic is development of innovative strategies to target solid tumor for therapy and imaging, based on EPR effect and nanotechnology; particularly focusing on the important molecule heme oxygenase-1 (HO-1) and its active product carbon monoxide (CO). He has published more than 60 papers in reputed journals and has been selected as a Thomson Reuters Highly Cited Researcher 2014, 2015.            
 

Abstract:

We previously reported the antitumor effect of heme oxygenase-1 (HO-1) inhibitor zinc protoporphyrin (ZnP), as well as its application for photodynamic therapy (PDT). Along this line, we synthesized a highly tumor targeting ZnPP micelle by conjugate HPMA polymer (pHPMA) to ZnP, which becomes highly water soluble and behaves as nano micelles in aqueous solution due to the hydrophobic interaction of ZnP, exhibiting mean hydrodynamic particle sizes of 82.8 nm. Accordingly, it exhibited significantly prolonged plasma half-life (t1/2>12h) and selective tumor accumulation by taking advantage of the enhanced permeability and retention (EPR) effect. pHPMA-ZnP alone did not show apparent cytotoxic effect, perhaps due to its slower intracellular uptake and thus lower HO-1 inhibition activity. However, a significant antitumor effect was found both in vitro and in vivo upon light irradiation, in different tumor models including autochthonous cancer. One dose of pHPMA-ZnP at 20 mg/kg (ZnP equivalent) administered I.V. followed by 2-3 times of light irradiation at an intensity of ≥20 J/cm² caused necrosis and disappearance of most tumors (>70%) in all tumor models. We also confirmed pHPMA-ZnP-based tumor imaging in autochthonous breast tumor in rat and mouse colon cancer models. The light dependent cytotoxicity was attributed to the generation of singlet oxygen. These findings warrant further development of pHPMA-ZnPP as an agent for PDT, and more important, as a fluorescent probe for tumor imaging due to its high tumor targeting property. The tumor distribution of pHPMA-ZnP micelles could be increased by concomitant application of vascular modulator like nitroglycerin.

Biography:

Naofumi Hashimoto received his PhD in Pharmaceutical Sciences from Kanazawa University. He began his research career at Shionogi Pharmaceutical Company in Japan in 1977. In 1999, he moved to Pfizer as a Manager of Pharmaceutical Sciences and was promoted to Research Advisor in 2004. He became Professor of Pharmaceutical Sciences of Setsunan University after Pfizer closed several research laboratories in the world. He has studied the application of nano-technologies to poor water soluble drug. He has published more than 30 papers and chapters in the areas of Pharmaceutical Sciences.

Abstract:

Nano-sizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds. Mebendazole (MBZ) is a well-known anthelmintic drug in wide clinical use. Recently, there were some reports that MBZ had the anticancer effect in preclinical study. However, the bioavailability of MBZ is low (<10%) due to poor solubility in water (ca. 0.5 µg/mL). The present investigation aimed to develop the nanocrystal formulations (about D₅₀=120 nm) of MBZ with improved dissolution behavior and thereby enhanced oral absorption.

Biography:

Josef Jampilek completed his PhD degree in Medicinal Chemistry at the Faculty of Pharmacy of the Charles University in 2004. During 2004-2011, he worked in expert and managerial posts in the R&D Division of the pharmaceutical company, Zentiva. In 2009, he became an Associate Professor of Medicinal Chemistry at the Department of Chemical Drugs at the Faculty of Pharmacy of the University of Veterinary and Pharmaceutical Sciences in Brno. He is an author/co-author of 27 patents, more than 120 peer-reviewed scientific publications, 7 university textbooks, 11 chapters in monographs and many invited lectures. He received several awards for his scientific results.

Abstract:

The vast majority of the known 2 million fungal species are strict saprophytes, but some of them can attack humans, animals and plants. It is estimated that 270,000 fungal species are associated with plants, and 325 fungal species, common in the environment, are known to infect humans. Human fungal infections range from superficial nail and skin infections to invasive, systemic infections that are really harmful to health and life. Human fungal infections generally receive less attention than bacterial and viral diseases, since the incidence of systemic fungal infections is considerably lower than that of superficial infections, however, mortality rates from invasive fungal infections are very high, often exceeding 50%, despite the use of antifungal drugs. Early diagnosis of disease and identification of the fungal pathogen remain crucial for the treatment of invasive fungal infections, because the efficacy of currently used drugs is limited by issues with administration route, narrow treatment window, activity spectrum, bioavailability, toxicity, drug resistance and cost. The increase in the number of fungal infections and the occurrence of new fungal opportunistic species is caused by general immunosuppression of the population. Agents can be divided into nonspecific antifungals and targeted site-specific antifungals.Although there is a relatively big number of topical antifungal medications, only about 12 drugs were approved for the treatment of systemic fungal infections (ATC J02A). Development of resistance/cross-resistance to commonly used drugs and multidrug-resistance of fungal pathogens constitute serious problems, and it is evident that new systemic (preferably orally administered) antifungal drugs are urgently needed.

Biography:

Siti Salwa Abd Gani has completed his PhD in 2010 from Universiti Putra Malaysia and Post-doctoral studies from School of Pharmacy, University College of London. She is a Senior Lecturer and Researcher at Universiti Putra Malaysia. He has published 20 papers in reputed journals and has been serving as a reviewer for several journals worldwide.      

Abstract:

In this study, the behavior of the caprylic and capric acids formulations containing octyl salicylate were investigated. The formulations were formulated using homogenization proses. The particle size, flow behavior, microscopic view and absorbance of the formulations were investigated. Particle sizes of the formulations were found in range 352.7 nm -704.2nm. The viscosity of the formulations changed as the shear rate was varied and could be classified as non-Newtonian fluids. The viscosity decreases when the fluid undergoes longer shear stress with time. The formulations containing octyl salicylate shows higher absorbance as compared to the formulations without octyl salicylate. The addition of octyl salicylate affected the system in terms of behavior, appearance and stability.

Biography:

Yusuf Ozkay has completed his PhD from Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry. He received Associate Professor Degree in 2012. He is the Vice Dean of Anadolu University Faculty of Pharmacy since April 2013. He has published more than 30 papers in reputed journals. Synthesis of new enzyme inhibitor candidates constitutes his main research area.

Abstract:

Alzheimer's disease (AD) a type of dementia that causes problems with memory, thinking and behaviour. Donepezil, an acetylcholinesterase (AChE) inhibitor, gives the most positive response to AD therapy. Donepezil carries indanone and piperidine ring systems on the structure. Thus, in the literature there are lots of studies including the synthesis and anticholinesterase activity investigation of these ring-systems or their bioisosters. Hence, this study was undertaken to synthesize new indan-1-one-piperazine derivatives and to evaluate their anticholinesterase activity. Chemical structures of synthesized compounds were confirmed by spectral data. Ellman’s assay was applied in order to investigate inhibitory potency of the compounds against Acetylcholinesterase (AChE) and Butrylcholinesterase (BChE) enzymes. It was determined that some of the compounds have significant activity on AChE. ADME (Absorption, distribution, metabolism, elimination) predictions were theoretically performed for all compounds in the series. Enzyme kinetics and molecular docking studies were carried out for the most active compound (2o) and nature of inhibition and interactions between enzyme and ligands were described.

Biography:

Mutlu Dilsiz Aytemir has completed her PhD at Hacettepe University in 2000 and done practical PhD studies at London University King’s College Department of Pharmacy from 1998 to 2000. She is a Lecturer at Hacettepe University from 2004 and become full professor in 2010. She has published 23 papers, 56 oral or poster presentation and a book chapter. Also, she is interested in medicinal chemistry in the field of synthesis of some Mannich bases that have antityrosinase, anti-aging, anticonvulsant, antiviral, antimicrobial, antitubercular, antioxidant and antimelanoma activities. She has incorporated Koji Cosmetic Chemistry Company in Türkiye. She will develop new dermocosmetic products having antityrosinase and anti-aging activities.

Abstract:

Kojic acid (5-hydroxy-2-hydroxymethyl-4H-pyran-4-one), the most intensively studied inhibitor of tyrosinase, was discovered in 1907. Since early twentieth century, it has been known as an additive to prevent browning of food materials such as crab, shrimp, and fresh vegetables in food industry (e.g., as an antioxidant or anti-browning agent) in order to preserve their freshness and to inhibit discoloration. Tyrosinase inhibitors can be used to prevent or treat melanin hyperpigmentation disorders. Therefore, nowadays, they have become increasingly important in medicine, cosmetics and food industries. They have found to have an important role in cosmetic industry for their skin lightening effect and depigmentation after sunburn. Kojic acid is currently used in tyrosinase inhibitors those are commercially available. Unfortunately, unstability during storage limits its use and new tyrosinase inhibitors of novel kojic acid derivatives are needed in cosmetics industry. More expended studies on this subject will be helpful in designing more suitable tyrosinase inhibitors for human use. Several natural or synthetic tyrosinase inhibitors have been discovered.  However, a few of them can be used as skin bleaching agents due to the toxicity problems. Development of high-performance tyrosinase inhibitors is currently needed for these fields. An object of the present invention is to synthesize new Mannich bases of kojic acid derivatives, which have better permeability than kojic acid and are not irritative, in high amounts and without by-product formation by means of a simple and efficient method that is conducted at room temperature. By increasing oil solubility of the obtained compounds, low permeability problem of the kojic acid is eliminated. 

Biography:

Vânia André has completed his PhD from University of Lisbon and currently a Post-doctoral fellow at Universities of Lisbon and Aveiro. She has published more than 50 papers in reputed international journals, 2 patents, 5 book chapters, 3 national publications and over 80 communications. She attended over 20 international schools/workshops/conferences to enrich her scientific knowledge and build a network of international scientists. Since 2006, she is focused on applying Crystal Engineering and Supramolecular Chemistry towards improving crystal forms of active pharmaceutical ingredients. Currently she is developing bio-inspired metal organic frameworks for enhanced drug storage, delivery and release

Abstract:

Nanoporours materials have attracted the interest of both academia and industry in various applications, the best known being gas storage, gas separation and shape/size selective catalysis.  Recently they started to be used in drug storage and delivery as well as in medical imaging and sensing. One of the most important challenges in drug delivery research is the efficient transport and release of drugs in the body using nontoxic nanocarriers to improve their activity and MOFs present the potential characteristics to solve this problem since they combine a high pore volume, a regular porosity and the presence of tunable organic groups within the framework, which allow the modulation of the structure of the framework as well as of the pore size. From a series of different active pharmaceutical ingredients (API) tested, results with nalidixic acid have shown to be promising. Nalidixic acid is a quinolone antibiotic used for the treatment of urinary tract infections, which can also act as bacteriostatic and as bactericidal. Bio-inspired networks of this API with safe metals are being successfully explored. Coordination with different metals, including Zn, Mn and Mg, yielded novel coordination networks. The use  of second ligands, such as oxalic and citric acids, has shown to be successful and it represents a pathway to obtain stuctures with higher porosity. Most of these new forms can be obtained by mechanochemistry, an efficient and environment-friendly synthetic technique.  The solubility and stability of these compounds sustents their viability for pharmaceutical applications.Nanoporours materials have attracted the interest of both academia and industry in various applications, the best known being gas storage, gas separation and shape/size selective catalysis.  Recently they started to be used in drug storage and delivery as well as in medical imaging and sensing. One of the most important challenges in drug delivery research is the efficient transport and release of drugs in the body using nontoxic nanocarriers to improve their activity and MOFs present the potential characteristics to solve this problem since they combine a high pore volume, a regular porosity and the presence of tunable organic groups within the framework, which allow the modulation of the structure of the framework as well as of the pore size. From a series of different active pharmaceutical ingredients (API) tested, results with nalidixic acid have shown to be promising. Nalidixic acid is a quinolone antibiotic used for the treatment of urinary tract infections, which can also act as bacteriostatic and as bactericidal. Bio-inspired networks of this API with safe metals are being successfully explored. Coordination with different metals, including Zn, Mn and Mg, yielded novel coordination networks. The use  of second ligands, such as oxalic and citric acids, has shown to be successful and it represents a pathway to obtain stuctures with higher porosity. Most of these new forms can be obtained by mechanochemistry, an efficient and environment-friendly synthetic technique.  The solubility and stability of these compounds sustents their viability for pharmaceutical applications.

Biography:

Professor at UIPS in Panjab University. She has published more than 80 research articles, has authored 1 book and has 6 patents to her credit. She has been awarded prestigious Commonwealth Academic Staff Fellowship for Post-doctoral studies at University of Strathclyde, UK. She is an active member of various professional bodies and has been designated as deputy coordinator of UGC -CAS programme of UIPS. Recently, she has published research in Chemical Reviews, a highest ranking journal in chemical sciences (Impact factor 45.6). She has been serving as an Editorial Board Member and reviewer of various journals of repute. Her areas of research interest include development of steroids and xanthines based new chemical entities of medicinal significance.

Abstract:

Adenosine receptors represent a new promising target for the development of various drug candidates for the treatment of a wide range of biological disorders. Currently four AR subtypes A₁, A_2A, A_2B and A₃ have been recognized and pharmacologically characterized. Adenosine A_2A receptor antagonism represents a novel non-dopaminergic approach in the treatment of Parkinson’s disease. Substituted xanthines represent the most potent class of adenosine receptor (AR) antagonists reported to date. Xanthine scaffold represents itself as a privileged motif, which offers numerous modifications at 1-, 3-, 7-, and 8-positions for the development of new potent and selective AR ligands. SAR studies have established that the structural modifications at 1- and 3-positions of the xanthine nucleus greatly affect the binding ability of the compounds for adenosine receptors. It has also been observed that the most remarkable alterations in potencies of the xanthines as antagonists of adenosine receptors result from appropriate substitution at the 8-position of this heterocyclic system. The current study describes a systematic approach to design and synthesize a new series of 1,3,7,8-tetrasubstituted xanthines as potent and selective adenosine A_2A receptor ligands for the treatment of Parkinson’s Disease.

Biography:

F Devrim Özdemirhan has completed her PhD from Middle East Technical University, Department of Chemistry. She is an Associate Professor at Abant Ä°zzet Baysal University. She is the MC (Management Committee) member at the CMST COST Action CM 1303 (System Biocatalysis). She has published more than 10 papers in reputed journals and has been serving as an Editorial Board Member of repute. 

Abstract:

Building blocks containing chiral tertiary alcohol frameworks is of great importance in  the field of pharmauchemistry and natural product industry. Oxygen involving, indan and tetralin compounds used to synthesize β-keto esters and antibiotic, i.e; thermorubin. Chemoenzymatic synthesis of optically active aromatic ring fused cyclic tertiary alcohols (S)-(-)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-ol, (S)-(+)-1-methyl-2,3 dihydro-1H inden-1-ol has been progressed. Lipases have been tried; CAL-A (C. a. Lipase A) was found to be the best biocatalyst for (±)-1-methyl-1,2,3,4 tetrahydronaphthalen-1-ol 1b and CAL-A-CLEA (Lipase A, C. a., cross-linked enzyme aggregate) for (±)-1-methyl-2,3-dihydro-1H-inden-1-ol, 1a, achieved with ee values of 20%, 45%, successively, the corresponding esters, 2b and 2a with the ee values  99 % , 71 % , respectively. Transesterification of (±)-1-methyl-2,3-dihydro-1H-inden-1-ol 1a and (±)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-ol 1b. The pharmaceutically active substances, a spirocycles make the synthesis and chemical reactivity of spiro cage an important area of research in organic. Cyclopent-2-ene barred tertiary allylic, homoallylic, homopropargylic alcohols, building blocks for spirocycles, have been resolved, via enzyme-catalyzed reaction with high ee (up to 90%) with 44%, 40% and 43% chemical yields, successively. The cyclohex-2-ene chain tertiary allyl, homoallyl and homopropargyl alcohols have been resolved in the same way at a high degree ee (up to 97 %) and in 42%, 45%, 49% chemical yields, sequentially. Enantiomerically enriched dienes from tertiary homoallyl alcohols related enantiomerically enriched spirocyclic dihydropyran compounds via RCM with 74% and 78% chemical yields and 90% and 97% ee, successively. Enantiomerically enriched enynes from tertiary homoallyl alcohols provided enantiomerically enriched cyclopentenone pyrans with spirocyclic motifs via PKR 80% and 81% chemical yields, respectively, as single diastereomers.

Biography:

Alexander J Andre Cobb is an Associate Professor of Organic Chemistry at the University of Reading. He started his career at King's College London where he studied Chemistry as an undergraduate. He then worked for his PhD at University College London under the guidance of Professor Charles Marson, investigating novel metal catalyzed asymmetric reactions. After completing this in 2001-02, he moved to the University of Cambridge to work briefly for Dr. Florian Hollfelder and then with Professor Steven V Ley CBE FRS in the fields of Organocatalysis and Medicinal Chemistry. In 2005, he was appointed to the faculty of the Reading School of Pharmacy and promoted to Associate Professor in October 2012.
 

Abstract:

The use of asymmetric organocatalysis as a method towards the construction of enantiopure molecules has burgeoned significantly in the last decade or so. Our group has developed several new reactions that lead to highly enantiopure biomolecules – mainly non-natural amino acids – using hydrogen bonding catalysis. We present the expedient synthesis of novel g- and d-amino acids, as well as other novel complex structures and derivatives, such as an analogue of the Amaryllidaceae alkaloid a-lycorane.

Biography:

Satyendra Kumar Pandey obtained his PhD degree in 2008 from the National Chemical Laboratory, Pune, India under the supervision of Dr. Pradeep Kumar. After working as a Post-doc student at the Purdue University, IN, USA, with Prof. Arun K Ghosh, he moved to Aurigene Discovery Tech. Ltd. (Dr. Reddy’s Lab) India, and joined as a Jr. Scientist in 2010. In 2012, he was appointed Assistant Professor in School of Chemistry and Biochemistry, Thapar University, India. He was the recipient of Eli Lilly Asia outstanding thesis award in 2009, and DST Young Scientist award in 2012. His broad research interests include development of new methodologies, synthesis of biologically active natural products, and medicinal chemistry.

Abstract:

Asymmetric synthesis of bioactive molecules is at the forefront of synthetic organic chemistry due to its varied applications in drugs and pharmaceutical industries. Among an array of naturally occurring and biologically important compounds, the functionalized amino acids, 2-alkyl substituted tetrahydroquinolines, 2,5-disubstituted-3-oxygenated THF motifs and α-phenyl-β²-amino acid core unit are of great importance. They possess interesting pharmacological properties such as antiepileptic, antimalarial, potent olfactory activities and significant cytotoxicity against a variety of tumour cell lines including L1210 murine leukaemia and KB human epidermoid carcinoma cells. As part of our research on the asymmetric syntheses of drugs and bioactive compounds, we have recently synthesized medicinally important antiepileptic drug (R)-lacosamide, antimalarial agent (+)-angustureine, (+)-petromyroxol with potent olfactory activities, (+)-serinolamide A having affinity and selectivity for the CB1 receptor, and (S)-nakinadine B with signicant cytotoxicity against a variety of tumour cell lines including L1210 murine leukaemia and KB human epidermoid carcinoma cells.¹

Biography:

Yusuf Ozkay has completed his PhD from Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry. He received Associate Professor Degree in 2012. He is the Vice Dean of Anadolu University Faculty of Pharmacy since April 2013. He has published more than 30 papers in reputed journals. Synthesis of new enzyme inhibitor candidates constitutes his main research area.

Abstract:

Alzheimer's disease (AD) a type of dementia that causes problems with memory, thinking and behaviour. Donepezil, an acetylcholinesterase (AChE) inhibitor, gives the most positive response to AD therapy. Donepezil carries indanone and piperidine ring systems on the structure. Thus, in the literature there are lots of studies including the synthesis and anticholinesterase activity investigation of these ring-systems or their bioisosters. Hence, this study was undertaken to synthesize new indan-1-one-piperazine derivatives and to evaluate their anticholinesterase activity. Chemical structures of synthesized compounds were confirmed by spectral data. Ellman’s assay was applied in order to investigate inhibitory potency of the compounds against Acetylcholinesterase (AChE) and Butrylcholinesterase (BChE) enzymes. It was determined that some of the compounds have significant activity on AChE. ADME (Absorption, distribution, metabolism, elimination) predictions were theoretically performed for all compounds in the series. Enzyme kinetics and molecular docking studies were carried out for the most active compound (2o) and nature of inhibition and interactions between enzyme and ligands were described.

Biography:

Mutlu Dilsiz Aytemir has completed her PhD at Hacettepe University in 2000 and done practical PhD studies at London University King’s College Department of Pharmacy from 1998 to 2000. She is a Lecturer at Hacettepe University from 2004 and become full professor in 2010. She has published 23 papers, 56 oral or poster presentation and a book chapter. Also, she is interested in medicinal chemistry in the field of synthesis of some Mannich bases that have antityrosinase, anti-aging, anticonvulsant, antiviral, antimicrobial, antitubercular, antioxidant and antimelanoma activities. She has incorporated Koji Cosmetic Chemistry Company in Türkiye. She will develop new dermocosmetic products having antityrosinase and anti-aging activities.

Abstract:

Kojic acid (5-hydroxy-2-hydroxymethyl-4H-pyran-4-one), the most intensively studied inhibitor of tyrosinase, was discovered in 1907. Since early twentieth century, it has been known as an additive to prevent browning of food materials such as crab, shrimp, and fresh vegetables in food industry (e.g., as an antioxidant or anti-browning agent) in order to preserve their freshness and to inhibit discoloration. Tyrosinase inhibitors can be used to prevent or treat melanin hyperpigmentation disorders. Therefore, nowadays, they have become increasingly important in medicine, cosmetics and food industries. They have found to have an important role in cosmetic industry for their skin lightening effect and depigmentation after sunburn. Kojic acid is currently used in tyrosinase inhibitors those are commercially available. Unfortunately, unstability during storage limits its use and new tyrosinase inhibitors of novel kojic acid derivatives are needed in cosmetics industry. More expended studies on this subject will be helpful in designing more suitable tyrosinase inhibitors for human use. Several natural or synthetic tyrosinase inhibitors have been discovered.  However, a few of them can be used as skin bleaching agents due to the toxicity problems. Development of high-performance tyrosinase inhibitors is currently needed for these fields. An object of the present invention is to synthesize new Mannich bases of kojic acid derivatives, which have better permeability than kojic acid and are not irritative, in high amounts and without by-product formation by means of a simple and efficient method that is conducted at room temperature. By increasing oil solubility of the obtained compounds, low permeability problem of the kojic acid is eliminated. 

Biography:

Abstract:

The development of new synthetic strategies for the synthesis of biologically active products  characterized by a reduced number of steps and high efficiency is an important goal in modern pharmaceutical chemistry. In this lecture, some particularly interesting examples of the synthesis of bioactive molecules realized in a multicomponent fashion starting from very simple and largely available building blocks, under mild and sustainanable conditions, will be illustrated, with special emphasis on catalytic processes. In particular, the catalytic syntheses of new heterocycles with antitumor activity (z-lactame, cyclic urea, spiro-isoindolinisoxazolidine and furofuranone derivatives), antibacterial activity (benzofurofuranone derivatives), and herbicidal activity (benzofuran, coumarin, and isobenzofuranimine derivatives) will be discussed.

Biography:

Professor at UIPS in Panjab University. She has published more than 80 research articles, has authored 1 book and has 6 patents to her credit. She has been awarded prestigious Commonwealth Academic Staff Fellowship for Post-doctoral studies at University of Strathclyde, UK. She is an active member of various professional bodies and has been designated as deputy coordinator of UGC -CAS programme of UIPS. Recently, she has published research in Chemical Reviews, a highest ranking journal in chemical sciences (Impact factor 45.6). She has been serving as an Editorial Board Member and reviewer of various journals of repute. Her areas of research interest include development of steroids and xanthines based new chemical entities of medicinal significance.

Abstract:

Adenosine receptors represent a new promising target for the development of various drug candidates for the treatment of a wide range of biological disorders. Currently four AR subtypes A₁, A_2A, A_2B and A₃ have been recognized and pharmacologically characterized. Adenosine A_2A receptor antagonism represents a novel non-dopaminergic approach in the treatment of Parkinson’s disease. Substituted xanthines represent the most potent class of adenosine receptor (AR) antagonists reported to date. Xanthine scaffold represents itself as a privileged motif, which offers numerous modifications at 1-, 3-, 7-, and 8-positions for the development of new potent and selective AR ligands. SAR studies have established that the structural modifications at 1- and 3-positions of the xanthine nucleus greatly affect the binding ability of the compounds for adenosine receptors. It has also been observed that the most remarkable alterations in potencies of the xanthines as antagonists of adenosine receptors result from appropriate substitution at the 8-position of this heterocyclic system. The current study describes a systematic approach to design and synthesize a new series of 1,3,7,8-tetrasubstituted xanthines as potent and selective adenosine A_2A receptor ligands for the treatment of Parkinson’s Disease.

Biography:

F Devrim Özdemirhan has completed her PhD from Middle East Technical University, Department of Chemistry. She is an Associate Professor at Abant Ä°zzet Baysal University. She is the MC (Management Committee) member at the CMST COST Action CM 1303 (System Biocatalysis). She has published more than 10 papers in reputed journals and has been serving as an Editorial Board Member of repute. 

Abstract:

Building blocks containing chiral tertiary alcohol frameworks is of great importance in  the field of pharmauchemistry and natural product industry. Oxygen involving, indan and tetralin compounds used to synthesize β-keto esters and antibiotic, i.e; thermorubin. Chemoenzymatic synthesis of optically active aromatic ring fused cyclic tertiary alcohols (S)-(-)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-ol, (S)-(+)-1-methyl-2,3 dihydro-1H inden-1-ol has been progressed. Lipases have been tried; CAL-A (C. a. Lipase A) was found to be the best biocatalyst for (±)-1-methyl-1,2,3,4 tetrahydronaphthalen-1-ol 1b and CAL-A-CLEA (Lipase A, C. a., cross-linked enzyme aggregate) for (±)-1-methyl-2,3-dihydro-1H-inden-1-ol, 1a, achieved with ee values of 20%, 45%, successively, the corresponding esters, 2b and 2a with the ee values  99 % , 71 % , respectively. Transesterification of (±)-1-methyl-2,3-dihydro-1H-inden-1-ol 1a and (±)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-ol 1b. The pharmaceutically active substances, a spirocycles make the synthesis and chemical reactivity of spiro cage an important area of research in organic. Cyclopent-2-ene barred tertiary allylic, homoallylic, homopropargylic alcohols, building blocks for spirocycles, have been resolved, via enzyme-catalyzed reaction with high ee (up to 90%) with 44%, 40% and 43% chemical yields, successively. The cyclohex-2-ene chain tertiary allyl, homoallyl and homopropargyl alcohols have been resolved in the same way at a high degree ee (up to 97 %) and in 42%, 45%, 49% chemical yields, sequentially. Enantiomerically enriched dienes from tertiary homoallyl alcohols related enantiomerically enriched spirocyclic dihydropyran compounds via RCM with 74% and 78% chemical yields and 90% and 97% ee, successively. Enantiomerically enriched enynes from tertiary homoallyl alcohols provided enantiomerically enriched cyclopentenone pyrans with spirocyclic motifs via PKR 80% and 81% chemical yields, respectively, as single diastereomers.

Biography:

Alexander J Andre Cobb is an Associate Professor of Organic Chemistry at the University of Reading. He started his career at King's College London where he studied Chemistry as an undergraduate. He then worked for his PhD at University College London under the guidance of Professor Charles Marson, investigating novel metal catalyzed asymmetric reactions. After completing this in 2001-02, he moved to the University of Cambridge to work briefly for Dr. Florian Hollfelder and then with Professor Steven V Ley CBE FRS in the fields of Organocatalysis and Medicinal Chemistry. In 2005, he was appointed to the faculty of the Reading School of Pharmacy and promoted to Associate Professor in October 2012.

Abstract:

The use of asymmetric organocatalysis as a method towards the construction of enantiopure molecules has burgeoned significantly in the last decade or so. Our group has developed several new reactions that lead to highly enantiopure biomolecules – mainly non-natural amino acids – using hydrogen bonding catalysis. We present the expedient synthesis of novel g- and d-amino acids, as well as other novel complex structures and derivatives, such as an analogue of the Amaryllidaceae alkaloid a-lycorane.

Biography:

Satyendra Kumar Pandey obtained his PhD degree in 2008 from the National Chemical Laboratory, Pune, India under the supervision of Dr. Pradeep Kumar. After working as a Post-doc student at the Purdue University, IN, USA, with Prof. Arun K Ghosh, he moved to Aurigene Discovery Tech. Ltd. (Dr. Reddy’s Lab) India, and joined as a Jr. Scientist in 2010. In 2012, he was appointed Assistant Professor in School of Chemistry and Biochemistry, Thapar University, India. He was the recipient of Eli Lilly Asia outstanding thesis award in 2009, and DST Young Scientist award in 2012. His broad research interests include development of new methodologies, synthesis of biologically active natural products, and medicinal chemistry.

Abstract:

Asymmetric synthesis of bioactive molecules is at the forefront of synthetic organic chemistry due to its varied applications in drugs and pharmaceutical industries. Among an array of naturally occurring and biologically important compounds, the functionalized amino acids, 2-alkyl substituted tetrahydroquinolines, 2,5-disubstituted-3-oxygenated THF motifs and α-phenyl-β²-amino acid core unit are of great importance. They possess interesting pharmacological properties such as antiepileptic, antimalarial, potent olfactory activities and significant cytotoxicity against a variety of tumour cell lines including L1210 murine leukaemia and KB human epidermoid carcinoma cells. As part of our research on the asymmetric syntheses of drugs and bioactive compounds, we have recently synthesized medicinally important antiepileptic drug (R)-lacosamide, antimalarial agent (+)-angustureine, (+)-petromyroxol with potent olfactory activities, (+)-serinolamide A having affinity and selectivity for the CB1 receptor, and (S)-nakinadine B with signicant cytotoxicity against a variety of tumour cell lines including L1210 murine leukaemia and KB human epidermoid carcinoma cells.¹

Biography:

Bhimapaka China Raju completed his PhD from Osmania University and Post-doctoral studies from Prof. H C Brown Center for Borane Research, Purdue University, USA. He is the Senior Scientist of CSIR-IICT, India a premier scientific organization. He has published 66 papers in reputed journals and has been serving as an Editorial Board Member of Oriental Journal of Chemistry, International Journal of Chemistry & Applications and E-Journal of Chemistry.

Abstract:

Heterocyclic compounds and their derivatives are important and are present in many biological systems. Among them, pyridine derivatives have found several applications in the pharmaceutical and agrochemical fields. Extensive studies have been carried out on synthesis of pyridine compounds because of their importance as drugs and natural products. Chloronicotinaldehydes are good precursors for the annulation of variety of heterocyclic analogues. Imidacloprid is the first chloronicotinyl insecticide, used worldwide for controlling pests due to its potency, broad spectrum of insecticidal activity with low mammalian toxicity. Our research group focused on 2-chloronicotinaldehyde based heterocyclic compounds, namely, Imidacloprid analogues, 2-chloro-5-methylpyridine-3-olefin derivatives, 1,8-naphthyridines, Baylis-Hillman (BH) adducts, 1H-1,2,3-triazolylbenzohydrazides, Knoevenagel derivatives, (E) α,β-unsaturated esters, ketones and studied their anti-microbial, anti-mycobacterial and anti-cancer activities. Further, we prepared various 1H-1,2,3-triazoles, 1H-1,2,3-triazolylisoxazoles and 1H-1,2,3-triazolyldihydroisoxazoles starting from 2-chloronicotinaldehydes in combination with TMP and screened for their anti-cancer and anti-tubulin properties. 

Biography:

Mrinalkanti Kundu is a Medicinal Chemist and carries 13 years of experience in small molecule therapeutics via orthosteric/allosteric modulation of GPCR, ion channels and enzymes with a track record in delivering pre-clinical candidates for metabolic disorders, pain, oncology and anti-infective programs. He completed his MSc and PhD from Indian Institute of Technology in Bioorganic Chemistry and was awarded Post-doctoral Fellowships in the field of Chemical Biology from University of Uppsala, National Institute on Aging, in collaboration with The Johns Hopkins University and University of Basel and published 10 patents, 15 articles and 1 book chapter.

Abstract:

DNA has played a key role as a molecular target for many of the drugs that have been used for decades in cancer therapeutics. Compounds that target DNA are some of the most effective agents in clinical use and produced increase in cancer patients’ survival but, they are extremely toxic. Consequently, enormous effort has been put into finding more selective agents; thus, there is considerable excitement in identifying cancer-specific DNA targets and thereby resulting in less toxic new therapeutics. This has driven interest in targeting unusual, non-canonical structures of DNA, in order to achieve selectivity while potentially reducing adverse side effects. Accordingly, cell-permeable specific probes targeting G-quadruplex structures should provide researchers with new tools for studying their potential involvement in gene expression, chromosome stability, viral integration and recombination. Significant research is in progress targeting G-quadruplex DNA with small molecules hoping to inhibit cancer growth according to two distinct mechanisms; first, promoter deactivation and second, inhibition of telomerase which is responsible for maintaining length of telomeres, and is involved in around 85% of all cancers. We wish to report the design, synthesis of novel drug-like small molecules and their biological evaluation as potential G-quadruplex stabilizing agents. Efficiency of these synthetic compounds for the stabilization of promoter quadruplex DNA structures was performed along with thorough investigation to assess the quadruplex binding affinity by using various biophysical and biochemical studies. For some of the compounds, the binding mode was explained by molecular modelling studies and their potential anti-cancer inhibitory effect was also tested.

Biography:

Chunduri Venkata Rao is currently a Professor of Chemistry in Sri Venkateswara University Tirupati. His area of research interest is Natural Products Chemistry and Synthesis of bioactive heterocyclic compounds. He has supervised 18 students for PhD and 6 for MPhil. At present 6 Research Scholars are working for their PhD Program. He has published over 70 research papers in national and international peer reviewed journals. He is a life member of ICC, Agra. He is serving as a reviewer and Editorial Board Member of reputed journals. In recent years he focused on the synthesis of various biologically active thieno & seleno pyrimidine derivatives.

Abstract:

Pyrimidines and fused pyrimidines are important classes of heterocyclic compounds that exhibit a broad spectrum of biological activities such as anticancer, antiviral, antibacterial, antioxidant, anti-inflammatory and analgesic activities. Among them quinazoline is the important scaffold which is an existing core moiety in gefitinib (as monotherapy for the treatment of patients with locally advanced or metastatic non-small cell lung cancer), lapatinib (as breast cancer treatment). Furthermore bioisosteric replacement of benzene ring in quinazoline by thiophene ring has been an important drug design strategy to optimize various lead structures like thienopyrimidines which shows the outstanding biological activities like Hsp90 ATPase Inhibitory, Tk Inhibitors DHFR inhibitory, CDK4 inhibitory, anti-inflammatory, anticancer and antitubercular activities. These thienopyrimidine  scaffolds also widely used in the drug discovery and have been employed broadly in the design of various kinase inhibitors, including cyclin-dependent kinase, phosphoinositide 3-kinase α(PI3Kα), EGFR/ErbB-2, aurora kinase and also implicated in the potential treatment or prevention of Alzheimer’s disease. Some substituted thieno [2,3-d] pyrimidines also act as a partial agonist for the luteinizing hormone/ choriogonadotropin receptor (LHCGR) and the closely related thyroid-stimulating hormone receptor (TSHR), the above literature survey and enormous importance of thienopyrimidines in present medicinal chemistry encouraged us to select the thienopyrimidine as our basic core moiety.  Hence in the present study a series of thienopyrimidine derivatives have been selected for the synthesis by incorporating the simple pharmacophores like oxadiazole, triazole, triazolothiadiazole, Schiff and Mannich bases and studied for their biological assay for in vitro microbial and cytotoxicity activity studies. All the compounds are well characterized by spectral data.

Biography:

Paulo Roberto Ribeiro Costa obtained his Post-doctoral studies at Université Joseph-Fourier (1984) and Université Paris-Sud (1988). He is Full Professor of Organic Chemistry at the Federal University of Rio de Janeiro since 1996 and has published more than 110 papers in reputed journals. He collaborated with several laboratories of the biological area in projects aiming the discovery of new bioactive compounds, especially isoflavonoid analogues with antiviral, antiparasitic and antineoplasic properties.

Abstract:

Isoflavanoids have being used in our laboratory as inspiration for the preparation of new compounds with antiviral, antiparasitic and antineoplastic activities. Several new 1-carbaisoflavanones, designed as analogues of bioactive natural isoflavanones, were prepared in environmentally appropriate conditions, by palladium catalyzed a-arylation of a-tetralones with o-bromoalkoxyphenols. Compound LQB-314 exhibited the best profile for HCV inhibition, being active in both replicon reporter cells (IC₅₀ 1.8 mM, SI > 111 in Huh7/Rep-Feo1b and IC₅₀ 4.3 mM, SI> 46 in Huh7.5-FGR-JC1-Rluc2A). Compound LQB-307 was the more potent and selective in Huh7.5-FGR-JC1-Rluc2A replicon reporter cells (IC₅₀ 1.5 mM, SI>101.4). Both compounds presented high bioselective index. Several of these substances have been converted in high yields into the corresponding 5-carbapterocarpens (total or partial demethylation of methoxy groups, followed by cyclization in a single step). These pterocarpens also showed potent anti-HCV activity. The best profile in Huh7/Rep-Feo1b replicon reporter cells was observed with LQB-359 (EC₅₀ 5.5 mM/SI 20), while LQB-418 was the most active in Huh7.5-FGR-JC1-Rluc2A replicon reporter cells (EC₅₀ 1.5 mM/SI 70). Hydroxy groups at A- and D-rings are essential for anti-HCV activity, and substitutions in the A-ring at positions 3 and 4 resulted in enhanced activity of the compounds.

Biography:

Sameer Agarwal has obtained Master’s in Chemistry from IIT, Delhi and was awarded DAAD (German Govt. Scholarship) fellowship to purse research project at Karlsruhe University, Germany. He has received PhD degree from Technical University, Dresden, Germany in the field of Synthetic and bio-organic chemistry under direction of Prof. Dr. Hans-Joachim Knölker, FRSC, a well-known scientist of present times for his contribution towards Alkaloid Chemistry. He worked as Research Scientist (Post-Doc), JADO Technologies, (collaboration with Max Planck Institute (MPI) of Molecular Cell Biology and Genetics and Chemsitry Department, Technical University), Germany. He then decided to return to his home country and working with Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad as Principal Scientist / Group Leader in the area of basic drug discovery and his research interest includes discovery of cardio metabolic, anti-inflammatory and oncology drugs. He has large number of publications in international journals and patents and is a reviewer of many prestigious journals including American Chemical Society. 

Abstract:

TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. In our pursuit of novel drugs with distinct mechanism of action for type 2 diabetes we report here the discovery of 2-((2-(4-(1H-imidazol-1-yl) phenoxy) ethyl)thio)-5-(2-(3,4-dimethoxyphenyl)propan-2-yl)-1-(4-fluorophenyl)-1H-imidazole as a novel, potent, selective and orally bioavailable TGR5 agonist. Using computer aided modeling studies we designed a series of novel 2-thio-imidazole derivatives, and then experimentally established a structure-activity relationship (SAR). The mentioned compound was identified as a TGR5 agonist with EC50 of 57pM and 62pM against the human TGR5 and mouse TGR5 receptors, respectively, in recombinant CRE-directed luciferase reporter gene assays. The compound showed a favorable pharmacokinetic profile. Further, this compound showed in vivo GLP-1 secretion in a C57 mouse model, and it potently reduced glucose excursion in oral glucose tolerance test (OGTT) in DIO C57 mice (ED50 = 7.9 mg/kg; ED90 = 29.2 mg/kg). 

Biography:

A novel series of 1-{[3-(furan-2-yl)-5-substituted phenyl-4,5-dihydro-1,2-oxazol-4-yl]methyl}-4-methyl piperazine, compounds 3a–l have been synthesized. The synthetic work was carried out beginning from 2-acetylfuran through Claisen Schmidt condensation with different types of aromatic aldehyde, affording 1-(furan-2-yl)-3-substituted phenyl prop-2-en-1-ones which on cyclization with hydroxylamine hydrochloride resulted in 3-(furan-2-yl)-5-substitutedphenyl-4,5-dihydro-1,2-oxazole formation. The isoxazolines were subjected to Mannich’s reaction in the presence of N-methyl piperazine to produce the desired products. The chemical structures of the compounds were proved by IR, ¹HNMR, ¹³CNMR and Mass spectrometric data. The antidepressant activity of the compounds was investigated by Porsolt’s behavioral despair (forced swimming) test on Albino mice. Moreover, the antianxiety activity of the newly synthesized compounds was investigated by the plus maze method. Compounds 3a and 3k showed the duration of immobility times of 152.00(s) and 152.33(s) respectively at 10 mg/kg dose level when compared to the standard drug imipramine (149.67s). Compounds 3a and 3k also showed significant antianxiety activity. A computational study for the prediction of ADME properties of the compounds was performed. It was encouraging to note that none of the compounds violated any Lipinski’s parameter. Lipophilicity data also suggested that compounds are lipophilic enough to cross blood brain barrier. The molecular modelling studies also predicted good binding interactions of most active molecules with MAO-A. 

Abstract:

Gita Chawla graduated in Pharmacy from College of Pharmacy, University of Delhi in 1987. Then, she did her MPharm in 1989 from Hamdard College of Pharmacy, University of Delhi and PhD in 1995 from Jamia Hamdard, New Delhi, India. She is Associate Professor in the Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India. Her field of specialization includes Medicinal Chemistry/Pharmaceutical Chemistry and Synthetic Chemistry. She has a teaching and research experience of around 21 years during which many students completed their MPharm research work under her guidance and submitted their MPharm theses and has guided PhD scholars also. She has authored numerous research publications in various journals of national and international repute. She has been serving as an Editorial Board Member in international journals of repute

Biography:

Poonam Piplani completed her PhD in the year 1997 and is currently holding the post of a Professor in the Institute. She has a teaching and research experience of over 24 years. She has 35 publications in the journals of both national and international repute and has attended various national and international conferences. She has two major research projects sanctioned by the University Grants Commission and Council of Scientific and Industrial Research, New Delhi. The Commonwealth Scholarship Commission, United Kingdom had selected her for the Commonwealth Academic Staff Fellowship, at the University of Starthclyde, Glasgow, UK. She has been included in the panel of PCI inspectors by the Pharmacy Council of India.

Abstract:

These days, dementia is a very costly burden on public health and an unmet medical need. Till date, many molecular targets such as acetylcholinesterase, phosphodiesterase, dopamine receptors, NMDA receptors, acetylcholine receptors etc. and behavioural pharmacological models have been studied for the discovery of new potential cognition enhancers. However, targeting inhibition of acetylcholinesterase has produced many clinically used block buster drugs. Piperazine is considered as a privileged structure as substitution at various positions of this nucleus results in a variety of derivatives possessing diversified biological properties. The functional importance of piperazine derivatives in cognition imposes very high requirements on their development as drug candidates. It was thus envisioned to synthesize some newer compounds having a better therapeutic profile by incorporating N₄ substituted piperazine ring and a substituted aryloxy moiety linked through various spacers in a single molecule. They will probably have the ability to interact with both the catalytic and the peripheral site of AChE, anticipating, the molecules may act as dual binding site AChE inhibitors. These compounds should be able to decrease the cognitive dysfunction and increase the cholinergic neurotransmission. Combining the chemical and pharmacological point of view, a series of novel piperazine derivatives has been designed, synthesized and evaluated for cognition improvement. All the synthesized compounds were evaluated as dual binding site inhibitors of acetylcholinesterase. The compounds encompassed an aryloxy moiety, a substituted piperazine and either a C-2 or C-3 spacer, so that they could interact with both the catalytic site and the peripheral anionic site (PAS) of acetylcholinesterase enzyme. The SAR study revealed that N-(4-{3-[4-(4-fluoro-phenyl)-piperazin-1-yl]-propoxy}-phenyl)-acetamide (I) containing the 4-(N-acetylamino)phenoxy and N₄-(p-fluorophenyl) piperazinyl moieties with a C-3 spacer was found to be the most active with IC₅₀ value 0.49 μM. Docking study showed that the carbonyl O-atom was involved in H-bonding with TYR130 and both the aromatic rings showed π-π stacking contact with Phe330, TRP84 and TRP279. In addition, the compound showed dual binding site inhibition and mixed type inhibition characteristics from enzyme kinetics studies. Furthermore, ex-vivo study exhibited CNS penetration ability, and was found to be active in passive avoidance memory evaluator model at a dose level of 1mg/kg. It also showed significant antiradical activity. Therefore, these evidences suggested that (I) could be developed as a prospective neuroprotectant and a cognition enhancer for the future pursuit. 

Biography:

Asunción Barbero studied Chemistry at the University of Valladolid and received her PhD degree at the same university working with Prof. Pulido. She then held Postdoctoral Fellowships at the University of Cambridge for two years working under the supervision of Prof. Ian Fleming in the study of stereocontrol in organic synthesis using silicon chemistry. She came back to Valladolid as Assistant Professor, was promoted to Associate Professor in 2001 and obtained the Spanish habilitation to full Professor in 2012. She has co-authored numerous international scientific publications and has delivered several invited and plenary lectures. Her current interests include the study of the silyl-cupration of multiple bonds and its application to the synthesis of natural and related products.

Abstract:

Biography:

Settypalli Triloknadh is currently doing PhD as UGC-SRF fellow under the supervision of Prof. C Venkata Rao in the Department of Chemistry, Sri Venkateswara University Tirupati, Andhra Pradesh, India. He has qualified national level Joint CSIR-UGC-JRF & NET exam under JRF category held in June-2011. He has attended several National & International conferences. He has been awarded the Prof. G L Talesara award-2014 for the Best Oral Presentation of his paper in Organic Chemistry Section in the 33^rd Annual National Conference of Indian Council of Chemists held at Department of Applied Chemistry, Indian School of Mines, Dhanbad during 15^th-17^th December, 2014. He has three years of research experience in organic synthesis towards the synthesis of heterocyclic compounds.

Abstract:

Thienopyrimidines occupy a special position among fused pyrimidines compounds these derivatives are characterized by a very broad spectrum of biological activities, such as antimicrobial, antiviral, anticancer, anti-inflammatory, antihistaminic, antipyretics, anticonvulsant, and immunostimulant properties. Along with some other pyrimidine systems containing an annulated five membered hetero aromatic ring, thienopyrimidines are structural analogs of biogenic purines and can be considered as potential nucleic acid antimetabolites. Various thienopyrimidine analogues attracted additional attention due to the broad spectrum of biological properties, they exhibited with a variety of annulations and functional group manipulations possible, some thieno[2,3-d]pyrimidine derivatives have shown interesting biological activity including as Hsp90 ATPase inhibitory, Tk inhibitors, DHFR inhibitory, CDK4 inhibitory activities. Furthermore various 1,2,4-triazole and their fused heterocyclic derivatives are also shows important biological properties like antimigraine, antiviral and analgesic activities. In addition fused heterocycle of1,2,4-triazole i.e., 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole also shows wide spectrum of biological activities including anti-fungal, antibacterial, antiviral, anthelmintic, antitumor, analgesic and anti-inflammatory activities. In view of their biological significance and in continuation of our ongoing research work to find out bioactive thienopyrimidines, the present work is an effort towards the synthesis and biological evaluation of some new 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole tagged thieno[2,3-d]pyrimidine derivatives. All the synthesized compounds are characterized by the spectral analysis. Docking and anti microbial activities of the synthesized are also studied.

Biography:

Sundaram Singh has completed her PhD from BHU, Varanasi. She is the Associate Professor of Chemistry Dept., IIT (BHU), Varanasi. She has published more than 20 papers in reputed journals. Her research area is green synthesis, organic synthesis and evaluation of biological activity. 

Abstract:

Multi-component reactions (MCRs), in which multiple reactions are combined into one synthetic operation, have been used extensively to form carbon-carbon bonds in synthetic chemistry. Such reactions offer a wide range of possibilities for the efficient construction of highly complex molecules in a single procedural step, avoid the complicated purification operations and allow savings of both solvents and reagents. In the past decade, there have been tremendous development in three- and four-component reactions and great efforts continue to be made to develop new MCRs. To date the development of new MCRs is an evolving and exciting research topic in organic synthesis, particularly in the synthesis of heterocyclic compounds. Superoxide chemistry is one of the most fascinating problems of current research. The use of this novel, innocuous and biochemical species has been demonstrated for achieving a number of organic transformations. Despite some progress made in the understating of the organic chemistry of superoxide ion, an important aspect involving the use of superoxide ion in multi-component synthesis still remains untouched and warrants study in this direction. The present report demonstrates a fast and selective multi-component transformation of an amines, cyclic 1, 3-diketone and aldehydes into benzothiazolo-/benzimidazolo-quinazolinone derivatives under mild reaction conditions of superoxide ion at room temperature in excellent yields. 

Biography:

Matthias D’Hooghe received a PhD degree in 2006 from Ghent University (Belgium) for his thesis entitled “2-(Bromomethyl)aziridines as versatile building blocks in organic chemistry”. In 2007, he became Post-doctoral Assistant at Ghent University, and in 2009 he performed a Post-doctoral stay at Eindhoven University of Technology (The Netherlands). In 2010, he was promoted to Research Professor at Ghent University, and was granted tenure in 2015. His main research interests include the chemistry of small-ring azaheterocycles and the synthesis of bioactive heterocyclic compounds. He received several awards and is the author of 117 publications in international peer-reviewed journals.

Abstract:

Small-ring azaheterocyclic systems have acquired a pivotal position as building blocks in medicinal chemistry. In particular, aziridines, azetidines and beta-lactams have been shown to be eligible synthons for the construction of a broad variety of stereodefined heterocyclic frameworks, often endowed with pronounced biological activities. In this presentation, the synthetic flexibility of these three- and four-membered systems toward the preparation of different types of pharmaceutically relevant nitrogen-containing target structures will be explained. In that respect, a number of novel synthetic strategies toward a broad set of important heterocyclic scaffolds will be discussed (see figure below). In particular, different new methods for the regio- and stereoselective rearrangement of aziridines, azetidines and beta-lactams into functionalized four- to seven-membered hetero (bi)cycles will be disclosed. All these compounds represent relevant moieties encountered as substructures in a variety of biologically active natural products and pharmaceuticals.

Biography:

Vânia André has completed his PhD from University of Lisbon and currently a Post-doctoral fellow at Universities of Lisbon and Aveiro. She has published more than 50 papers in reputed international journals, 2 patents, 5 book chapters, 3 national publications and over 80 communications. She attended over 20 international schools/workshops/conferences to enrich her scientific knowledge and build a network of international scientists. Since 2006, she is focused on applying Crystal Engineering and Supramolecular Chemistry towards improving crystal forms of active pharmaceutical ingredients. Currently she is developing bio-inspired metal organic frameworks for enhanced drug storage, delivery and release. 

Abstract:

Nanoporours materials have attracted the interest of both academia and industry in various applications, the best known being gas storage, gas separation and shape/size selective catalysis.  Recently they started to be used in drug storage and delivery as well as in medical imaging and sensing. One of the most important challenges in drug delivery research is the efficient transport and release of drugs in the body using nontoxic nanocarriers to improve their activity and MOFs present the potential characteristics to solve this problem since they combine a high pore volume, a regular porosity and the presence of tunable organic groups within the framework, which allow the modulation of the structure of the framework as well as of the pore size. From a series of different active pharmaceutical ingredients (API) tested, results with nalidixic acid have shown to be promising. Nalidixic acid is a quinolone antibiotic used for the treatment of urinary tract infections, which can also act as bacteriostatic and as bactericidal. Bio-inspired networks of this API with safe metals are being successfully explored. Coordination with different metals, including Zn, Mn and Mg, yielded novel coordination networks. The use  of second ligands, such as oxalic and citric acids, has shown to be successful and it represents a pathway to obtain stuctures with higher porosity. Most of these new forms can be obtained by mechanochemistry, an efficient and environment-friendly synthetic technique.  The solubility and stability of these compounds sustents their viability for pharmaceutical applications.

Biography:

Dominic Ormerod is a Senior Researcher in the Green Chemical Technology group at VITO, which he joined in February 2012. After obtaining a PhD in Organic Chemistry, (1998, Univesité Catholique de Louvain, Louvain-La-Neuve Belgium) in the group of Prof. I. E. Markó, he moved to Janssen Pharmaceutica, Beerse, Belgium in the Department of Chemical Process Development, where he worked from 1998 until January 2012. In his current role, he Leads research directed towards membrane assisted process intensification. He is the author of 14 publications and inventor on 9 patents.

Abstract:

Successful chemical production of molecules whilst simultaneously reducing the environmental impact of the process relies not only on more efficient reactions but also on developments in reactor and separation technology. Recent decades have also witnessed a significant growth in industrial interest in solvent based separations using membranes stable to organic solvents. Thanks to its non-thermal, hence mild and energy-efficient character, organic solvent nanofiltration (OSN) is capable of efficiently concentrating and purifying valuable target molecules, removing post-reaction residues and recovery of spent solvents or catalysts. Furthermore, process intensification can be achieved by the integration of OSN with chemical reactions, resulting in significant gains in purity and/or capacity, and concomitant decreases in energy demand, raw material usage and/or waste volumes. One particular development deals with reactions which require, for various reasons, a high substrate dilution in order to avoid the formation of unwanted secondary products. This results in large volumes of solvent being necessary to produce relatively small quantities of the desired molecule. A typical case where such diluted conditions are required is the synthesis of macrocyclic molecules. Despite this drawback, globally several macrocyclic compounds are being produced on an industrial scale, however in a very inefficient manner. In order to address the economic and environmental shortcomings of high dilution reactions, VITO has developed a processing method that incorporates in line solvent recycling via OSN. This membrane-assisted methodology allows for significant reductions in the solvent load without loss in product yield or analytical purity as compared to a batch process. In collaboration with industrial partners, the potential of this novel methodology has been demonstrated in the preparation of numerous macrocyclic molecules.

Biography:

Anna Maria Waszkielewicz defended her PhD in 2008 in Medicinal Chemistry. She has published more than 35 papers in reputed journals (overall IF>60) and has been serving as an Editorial Board Member of repute Organic Chemistry – Current Research as well as Jacobs Journal of Organic Chemistry. She was granted patents for new drug candidates in US, EPO, Russia, Japan, Canada, Korea, and Poland. She has coordinated cooperation between National Cancer Institute and Jagiellonian University Medical College in discovery of anticancer agents. She is an Assistant Professor at Department of Bioorganic Chemistry, Chair of Organic Chemistry, Jagiellonian University Medical College, Poland.

Abstract:

The aim of the study was determination of correlation between activities: anticonvulsant, analgesic, antidepressant and anxiolytic, among novel compounds, as well as finding mechanism of action of these compounds. Premise for the above aim constitutes coexistence and common etiology of these disorders, such as trauma, intoxication, or neurodegeneration. Among epilepsy patients, morbidity in migraine is 2.4 times as high as between patients who have no seizures. 20-50% of epilepsy patients suffer from depression. Special situation is observed for patients such as children or pregnant women, as well as those who suffer from drug-resistant epilepsy. It is known that anticonvulsants such as carbamazepine, valproates, or gabapentin improve mood and that tianeptine may cause depression. On the other hand, epilepsy can be caused by maprotyline and klomipramine. Drugs such as venlafaxine and selective serotonin reuptake inhibitors are considered relatively safe. Based on our experience regarding aroxyalkyl- and aroxyethoxyethylaminoalkanols and their anticonvulsant and analgesic activity, new phenoxyalkyl and phenoxyethoxyethyl derivatives of piperazine have been designed and synthesized for in vivo screening for epilepsy (maximal electroshock, MES), neurotoxicity (rotarod), antidepressant-like activity (Porsolt test), as well as anxiolytic activity (four-plate test) have been examined. Receptor profile for the compounds has been determined. As an additional assay, mutagenic activity was excluded. Moreover, metabolic stability was determined with use of murine liver microsomes for the most active compounds.

Biography:

Sahar Ahmed is an Assistant Professor at the Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, KSA. She received her BSc from the Faculty of Pharmacy, Assiut University, Egypt and then her MSc from the same faculty. She subsequently obtained her PhD from the Faculty of Pharmacy, University of Alberta, Canada in 2010 under the supervision of Dr. K Kaur followed by one year of a Post-doc at the same faculty. She has participated in many international conferences and published 15 publications in international journals and one chapter book.

Abstract:

An in-vitro platform to perform a peptide screening against different cancer cell lines was designed. The strategy for this screening relied on detection of high affinity cancer targeting peptides based on the sequence of NGR and P160. Evaluation of the best binding peptides was done through incubation of the cellulose membrane-bounded cells with MTT reagent which is reduced to purple formazan in living cells, further quantified using Elispot and Kodak imager. For a proof of concept, a peptide library (132 spot, 66 different peptides) was designed, synthesized, and screened against different cancer cell lines. Current screening process assist in the identification of positive, negative peptide, and the relative binding between positive ones. Better binding peptides of NGR sequence were pointed out to show up to 2.6 fold increase to CD13 positive cell lines with insignificant binding to CD13 negative ones. Comparable results were observed for P160 sequences where different peptides showed higher binding up to 3 fold increase relative to the native P160 peptide. Based on our results, an alternative colour approach to identify new peptides for cancer targeting was developed and applied for two different peptide libraries.

Biography:

Flavio S P Cardoso obtained a BS degree in Chemistry in 2009 at the State University of Campinas (UNICAMP), Brazil. He performed undergraduate research under the supervision of Prof. Carlos Roque Duarte Correia for a period of nearly three years. His research at UNICAMP focused on the palladium-catalyzed Heck-Matsuda reaction. Next, he started his graduate studies at the University of Florida, USA. Under the guidance of Prof. Aaron Aponick, his PhD studies involved the development of a new class of atropisomers which was ultimately applied in asymmetric catalysis. Upon graduation in 2014, he moved back to Brazil to work at Libbs Pharmaceuticals as a Chemical Development Scientist.

Abstract:

An efficient synthesis of 17-α-estradiol 1 is described. Utilization of in situ IR allowed for an online monitoring of the key Mitsunobu reaction and development of a safe and reliable synthesis of 17-α-estradiol 1 in 78% overall yield over three steps. Benzoylation of 17-β-estradiol 2 is conducted at high regioselectivity under phase-transfer catalysis (PTC) conditions, followed by a Mitsunobu reaction to invert the chiral center at C-17 and provide intermediate 5, containing the core structure of 17-α-estradiol 1. Finally, the desired active pharmaceutical ingredient (API) is prepared by saponification of the remaining esters.

Biography:

Nafiz Oncu Can has completed his PhD from Anadolu University under the supervision of Prof. Dr. Goksel ARLI. He has published 15 papers in reputed journals and has an H-index value of 7. He is working as a full-time Associate Professor at the Department of Analytical Chemistry, Faculty of Pharmacy, Anadolu University, Turkey.

Abstract:

Avanafil (AVA) is a phosphodiesterase type 5 inhibitor compound, prescribed to treat erectile dysfunction. Up to date, due to recent introduction of AVA to the market, chemical analysis of its degradation products and possible process impurities were not published anywhere. A novel reversed-phase high-performance liquid chromatography method was developed and validated for the determination of avanafil, in the presence of its degradation products. Forced degradation studies were performed employing acidic, alkaline, neutral, oxidative, thermal and photolytic stress conditions and retention characteristics of AVA was assessed by the evaluation of common chromatographic and system suitability parameters. Identification of compounds was realized using LCMS-IT-TOF instrument and an additional LC-MS/MS system was utilized for precise quantitation of AVA. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to specificity, accuracy, precision, linearity, limit of detection and quantification, and robustness. The applicability of the proposed method for the determination of avanafil was demonstrated.

Biography:

Karem H Alzoubi, PhD, Professor of Pharmacology, Dean of the Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan. He has published over 160 peer-reviewed research articles and review article in well-respected international journals, and a number of book chapters. He presented his work in over 50 international conferences all over the world. His scientific work has been highly cited. He has a current, Scopus h index of 24, which is the highest among researchers in Jordan and among the highest in the Arab world in the fields of pharmacy/pharmacology. He was awarded Khalifah Award for Education (an international award) distinguished University Professor in the Field of Scientific Research from Government of United Arab Emirates (UAE) (2014-2015). He also won the Abdul-Hameed Shoman Young Arab investigators Award for Medical Sciences for 2012 from the Shoman forum. He was also awarded the Distinguished Researcher Award in the fields of Medicine and Pharmacy from the Ministry of Higher Education and Scientific Research, Amman, Jordan (2013).

Abstract:

Herbal medicinal products represent a major focus for drug development and industry and it holds a significant share in drug-market all over the globe. Recently, a number of medicinal plant extracts from Jordan with high antioxidative capacity were shown for their protective effect against DNA damage, which correlates future likelihood of cancer development or birth defects. In this study, we evaluated plant extract with high antioxidative DNA damage properties for anti-mutagenic effect using sister chromatid exchange assay in cultured human lymphocytes. As per our screening results, plant extracts with antioxidative DNA damage properties were the hexane fraction of Silybum marianum L. (aerial parts), the chloroform fractions of Pistacia palaestina Boiss (Fruits), the ethanolic fractions of Salvia triloba L. (leaves), Ziziphus spina-christi L. Desf. (Fruits/leaves) and Eucalyptus camaldulensis Dehnh (leaves). These plant extract fractions were further analyzed using sister chromatid exchange assay in cultured human lymphocytes. Results showed that the ethanolic fractions of spina-christi L. Desf. (Fruits/leaves), and Eucalyptus camaldulensis Dehnh (leaves) significantly reduced the rate of sister chromatid exchanges in cultured human lymphocytes at doses of 100 ug/ml, 500 ug/ml. Additionally, the hexane fraction of Silybum marianum L. (aerial parts) significantly reduced the rate of sister chromatid exchanges in cultured human lymphocytes at a dose of 500 ug/ml. These results indicate the antimutagenic activity of the ethanolic fractions of spina-christi L. Desf. (Fruits/leaves), Eucalyptus camaldulensis Dehnh (leaves) and hexane fraction of Silybum marianum L. (aerial parts); and thus, their increased potential as cancer protective agents.

Biography:

Gary Gellerman has completed his PhD from Tel Aviv University in 1994 and joined Compugen Ltd. In 2000, he accepted the position of Vice-president, Molecular Diversity in Compugen where he was responsible for developing drug discovery platform. In 2005, he moved to Ariel University, currently holding Deanship of Faculty of Natural Sciences. He has published more than 50 articles in reputed journals.

Abstract:

Resistance to drugs that cancer cells develop and the inherent capability of these cells to survive the drug treatment, produces a great motivation to look for new techniques of chemotherapeutic cure and search for novel anti-proliferative agents. In the present report, we demonstrate a facile synthetic strategy towards the discovery of new anti-cancer substances. This strategy is based on simple covalent coupling between known anti-cancer drugs, which results in novel 'chimeric' small molecules. One of the novel compounds presented here, CM358, is a result of amide bond formation between known Topo II inhibitor amonafide (AM) and DNA mustard alkylator chlorambucil (CLB). It demonstrates a significant cytotoxic predominance over the equimolar mixture of AM and CLB in various cancer cell lines and in xenograft model of human metastatic melanoma. Modeling studies and FACS analysis of CM358 will also be presented. 

Biography:

Garcinia atroviridis is a medium-sized fruit tree found wild in the forest of Peninsular Malaysia, Thailand, Myanmar, India and sometimes in a half-cultivated state in villages. It is commonly known as ‘Asam Gelugor’ in Malaysia or ‘Som-Khaek’ in Thailand. G. atroviridis has been used as a postpartum medication agent in folkloric medicine. The fruit is used in a lotion made with vinegar, which is rubbed upon the abdomen of a woman after confinement and the juice from the leaves is given to a woman after childbirth in one of those numerous protective preparations. In the investigation on the chemical constituents of the stem bark of G. atroviridis, eleven compounds have been isolated and purified using column chromatography. These compounds were characterized using various spectroscopic techniques and were assayed for antioxidant and cholinesterase enzyme inhibitory activities. 

Abstract:

Wen-Nee Tan has completed her PhD in Natural Products Chemistry from Universiti Sains Malaysia and is currently a Lecturer in Universiti Sains Malaysia. Her research interests focus on natural products isolation and their structural characterization, as well as bioassay on the isolated pure compounds.