Medicinal Chemistry For Practitioners

Presenting both a panoramic introduction to the essential disciplines of drug discovery for novice medicinal chemists as well as a useful reference for veteran drug hunters, this book summarizes the state-of-the-art of medicinal chemistry. It covers key drug targets including enzymes, receptors, and ion channels, and hit and lead discovery. The book hen surveys a drug's pharmacokinetics and toxicity, with a solid chapter covering fundamental bioisosteres as a guide to structure-activity relationship investigations.

Completely revised and updated, the 2nd edition of The Handbook of Medicinal Chemistry draws together contributions from authoritative practitioners to provide a comprehensive overview of the field as well as insight into the latest trends and research. An ideal companion for students in medicinal chemistry, drug discovery and drug development, while also communicating core principles, the book places the discipline within the context of the burgeoning platform of new modalities now available to drug discovery. The book also highlights the role chemistry has to play in wider target validation and translational technologies. This is a carefully curated compilation of writing from global experts using their broad experience of medicinal chemistry, project leadership and drug discovery and development from an industry, academic and charity perspective to provide unparalleled insight into the field.

Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.

CONTEMPORARY ACCOUNTS IN DRUG DISCOVERY AND DEVELOPMENT A useful guide for medicinal chemists and pharmaceutical scientists Drug discovery is a lengthy and complex process that typically involves identifying an unmet medical need, determining a biological target, chemical library screening to identify a lead, chemical optimization, preclinical studies and clinical trials. This process often takes many years to complete, and relies on practitioners’ knowledge of chemistry and biology, but also—and perhaps more importantly—on experience. Improving the success rate in discovery and development through a thorough knowledge of drug discovery principles and advances in technology is critical for advancement in the field. Contemporary Accounts in Drug Discovery and Development provides drug discovery scientists with the knowledge they need to quickly gain mastery of the drug discovery process. A thorough accounting is given for each drug covered within the book, as the authors provide pharmacology, drug metabolism, biology, drug development, and clinical studies for every case, with modern drug discovery principles and technologies incorporated throughout. Contemporary Accounts in Drug Discovery and Development readers will also find Case histories used as an engaging way of learning about the drug discovery/development process Detailed biological rational and background information, drug design principles, SAR development, ADMET considerations, and clinical studies The full history of individual marketed small molecule drugs Coverage of drug candidates that have passed Phase I clinical trials with different modalities, such as antibody drug conjugates (ADC), proteolysis-targeting chimera (PROTAC), and peptide drugs The application of new technologies in drug discovery such as DNA-encoded libraries (DEL), positron emission tomography (PET), and physics-based computational modeling employing free energy perturbation (FEP) Contemporary Accounts in Drug Discovery and Development is a helpful tool for medicinal chemists, organic chemists, pharmacologists, and other scientists in drug research and process development. It may be considered essential reading for graduate courses in drug discovery, medicinal chemistry, drug synthesis, pharmaceutical science, and pharmacology. It is also a useful resource for pharmaceutical industry labs, as well as for libraries.

An introduction to medicinal chemistry including computing and other modern techniques. The main objective of medicinal chemistry is the design and synthesis of new medicines, and this book covers widely this rapidly developing and important field of chemistry.

The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry highlights the necessity for an integrative approach in medicinal chemistry and chemical biology. As medicinal chemistry is not a monolithic science, it is important to emphasize the other various disciplines that are required for successful drug design. This book presents the author’s own personal experience in this field and describes the "ups" and "downs" that come with drug discovery. It is an excellent companion text for graduate and postgraduate students who would like further insight into the parameters of drug design, including the challenges that come with the project. Key Features Illustrates "real-life" examples in medicinal chemistry Integrates the use of physical, chemical, and biological concepts that are important in drug design Highlights the "ups" and "downs" that come with drug discovery Aims to inspire students who may be struggling with the challenges and thought process in drug design Intends to be an excellent companion text for graduate and postgraduate students

Medicinal chemistry is a complex topic. Written in an easy to follow and conversational style, Basic Concepts in Medicinal Chemistry focuses on the fundamental concepts that govern the discipline of medicinal chemistry as well as how and why these concepts are essential to therapeutic decisions. The book emphasizes functional group analysis and the basics of drug structure evaluation. In a systematic fashion, learn how to identify and evaluate the functional groups that comprise the structure of a drug molecule and their influences on solubility, absorption, acid/base character, binding interactions, and stereochemical orientation. Relevant Phase I and Phase II metabolic transformations are also discussed for each functional group. Key features include: • Discussions on the roles and characteristics of organic functional groups, including the identification of acidic and basic functional groups. • How to solve problems involving pH, pKa, and ionization; salts and solubility; drug binding interactions; stereochemistry; and drug metabolism. • Numerous examples and expanded discussions for complex concepts. • Therapeutic examples that link the importance of medicinal chemistry to pharmacy and healthcare practice. • An overview of structure activity relationships (SARs) and concepts that govern drug design. • Review questions and practice problems at the end of each chapter that allow readers to test their understanding, with the answers provided in an appendix. Whether you are just starting your education toward a career in a healthcare field or need to brush up on your organic chemistry concepts, this book is here to help you navigate medicinal chemistry. About the Authors Marc W. Harrold, BS, Pharm, PhD, is Professor of Medicinal Chemistry at the Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA. Professor Harrold is the 2011 winner of the Omicron Delta Kappa "Teacher of the Year" award at Duquesne University. He is also the two-time winner of the "TOPS" (Teacher of the Pharmacy School) award at the Mylan School of Pharmacy. Robin M. Zavod, PhD, is Associate Professor for Pharmaceutical Sciences at the Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, where she was awarded the 2012 Outstanding Faculty of the Year award. Professor Zavod also serves on the adjunct faculty for Elmhurst College and the Illinois Institute of Technology. She currently serves as Editor-in-Chief of the journal Currents in Pharmacy Teaching and Learning.

Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.