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Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. - New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations - Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years - Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in che...
Volume 5 of Advances in Medicinal Chemistry contains four intriguing and detailed accounts of the close interface between synthetic chemistry, structure-activity relationships, biochemistry, and pharmacology. In Chapter 1, there is a comprehensive survey of the immunophilin area specifically focussing on neuroregenerative applications in the central nervous system. In Chapter 2, there is an overview of the development of a potent analgesic compound that works via modulation of neuronal nicotinic acetylcholine receptors. In Chapter 3, there is a description of dopamine D-2 autoreceptor partial agonists as potential therapy for the treatment of schizophrenia. In Chapter 4, there is a summary of the successful program in which potent non-peptide inhibitors of HIV protease from the AIDS virus were developed.
Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment ...
This two volume book is an excellent introduction to this interdisciplinary area, lying on the interface between organic chemistry, biochemistry and medicine. The authors give a comprehensive overview of the field and outline the actual challenges in pharmaceutical science and industry. Volume 1 introduces the concepts of drug design and drug metabolic processes as well as antibacterial, antiviral and anticancer agents.
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A slow and consistent study of the approaches for drug design can help the foundation for a good scientific intuition. This edition includes over 30 new illustrations, numerous new mechanistic schemes and enhanced original figures. In addition, the use of color makes its study more pleasant and impressive. The Second Edition has been thoroughly revised with a modern look. The chapters on QSAR and Drug Metabolism have been extended, emphasizing concepts, such as the hyperconjugative effect or the anomeric effect, in which the student normally finds it difficult to understand. Stereoelectronic effects are essential to explain the mechanism of action of drugs and therefore, its agile and intuit...