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