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The past fifteen years have seen a revolution in the field of stereochemistry, with breakthrough analytical techniques in enantiomeric separation profoundly affecting drug development and use. This practical reference written by leading researchers focuses on the important roles chirality and stereoisomerism play in drug development efforts--presenting for the first time a comprehensive overview of this rapidly evolving area of pharmacological research. The book explores analytical, pharmacological, and regulatory topics in dealing with the theory and practice of stereochemistry in the pharmaceutical industry today. This exciting, broad-appeal treatment extends from the analytical viewpoint in enantiomeric separation to the regulatory issues involved in the "racemate-versus-enantiomer" debate. The authors include numerous examples and case studies, and integrate material from a wide range of studies, publications, and workshops. The introductory chapters outline the pharmacological effects of stereochemistry, cover stereochemistry in drug metabolism, and discuss problems inherent in the duality of enantiomers--chemically identical yet spatially different molecules. Contributions on the specific aspects of chirality and drug activity explore the toxicological effects of stereoselectivity, illustrate how an understanding of the stereochemical composition of certain drugs can help avoid problems, and offer tips on new clinical applications for existing drugs. A full chapter is devoted to research opportunities in the development of new chirally pure drugs. Other practical research topics range from the preparation of chirally pure compounds to the analytical determination of stereochemical composition, to applications of circular dichroism (CD) spectroscopy. Regulatory issues concerning the development and approval of stereoisomeric drugs are discussed in the final chapters. This section offers an international perspective as well as a historical review of the ongoing debate surrounding regulatory guidelines. Impact of Stereochemistry on Drug Development and Use is an essential reference for medicinal and analytical chemists, pharmacologists, drug metabolism and pharmacokinetic scientists, and personnel of regulatory agencies. It is also a useful text for graduate students in stereochemistry, and for anyone who wants to keep up with the swift pace of change in this dynamic field. Impact of Stereochemistry on Drug Development and Use is an essential reference for medicinal and analytical chemists, pharmacologists, drug metabolism and pharmacokinetic scientists, and personnel of regulatory agencies. It is also a useful text for graduate students in stereochemistry, and for anyone who wants to keep up with the swift pace of change in this dynamic field. IMPACT OF STEREOCHEMISTRY ON DRUG DEVELOPMENT AND USE Twenty-three expert contributions on the "stereochemical revolution" of the last fifteen years--covering analytical, pharmacological, and regulatory topics--show that "drug development can no longer occur without consideration of drug stereochemistry." "We have...come full circle and stand alongside Pasteur in amazement of nature's duality, symmetry and dissymmetry, and its chemical and pharmacological consequences."--from the Preface
Covering every essential element in the development of chiral products, this reference provides a solid overview of the formulation, biopharmaceutical characteristics, and regulatory issues impacting the production of these pharmaceuticals. It supports researchers as they evaluate the pharmacodynamic, pharmacokinetic, and toxicological characteristics of specific enantiomers and chiral drug compounds and addresses in one convenient reference all the major challenges pertaining to drug chirality that have been neglected in the literature. Chirality in Drug Design and Development collects the latest studies from an interdisciplinary team of experts on chiral drug design.
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
Maintaining and enhancing its focus on key issues in the development, regulatory approval and use of stereoisomeric compounds, this edition continues to cover in detail all aspects of chiral drugs from the academic, governmental, industrial and clinical points of view.;Completely rewritten and updated throughout, Drug Stereochemistry: illustrates current indirect chromatographic methods for the resolution of drug enantiomers; treats the rapidly growing area of enantioselective gas chromatography; discusses the latest in HPLC resolution of enantiomeric drugs; uses verapamil as a model to show how stereoselective pharmacokinetics affect pharmacodynamics; and supplies an in-depth study on the effect of stereoselective plasma protein binding.;This edition offers entirely new chapters that: discuss the recent decisions and present position of the US Food and Drug Administration on the development of stereoisomeric drugs; explicate enzymatic synthesis of stereochemically pure drugs; review the toxicological, pharmacokinetic and pharmacodynamic differences found among stereoisomers; elucidate the stereoselective transport of drugs across epithelia; and give a physician's perspective on the questions and problems caused by stereoisomeric drugs in practice as well as the pharmaceutical industry's collective viewpoint based on a national survey.
The most concise and streamlined textbook available on organic chemistry for the pharmacy student Organic Chemistry for Pharmacy is a textbook written specifically for the students taking the required Organic/Medical Pharmacy course. Using a building-block approach, the book delivers a basic, yet thorough discussion of the mode of action, therapeutic applications, and limitations of various pharmaceutical agents. Organic Chemistry for Pharmacy is especially written for students who have a limited background in chemistry. In order to make the learning/teaching experience as efficient as possible, Organic Chemistry for Pharmacy includes outstanding pedagogical features such as chapter outlines, chapter summaries, boxed “take away points”, quick-reference tables, and problems within each chapter. The focus and presentation of this text is particularly suited for Organic/Medical Pharmacy courses which are weighted heavily towards Organic, rather than Medical Pharmacy.
Drug Stereochemistry: Analytical Methods and Pharmacology, Third Edition covers all aspects of chiral drugs from academic, governmental, industrial, and clinical perspectives, reflecting the many advances in techniques and methodology. Topics include:The use of enzymes in the synthesis and resolution of enantiometrically pure compounds in drug disc
Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.
This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.
The volume contains the main papers presented at the 1994 EUROTOX Congress, Basel, Switzerland, August 21-24, 1994. Toxicology has become a less descriptive science because more importance has been placed on the mechanisms underlying toxic effects. This is reflected in symposia and workshops devoted to species differences in organ toxicity, receptor-mediated toxicity and stereochemical effects of xenobiotics. Recent progress in the fields of immunotoxicology, ecotoxicology, and neurotoxicology is highlighted and documented together with the present discussion on harmonized regulatory guidelines.
This unique book stands as the only comprehensive introduction to vibrational optical activity (VOA) and is the first single book that serves as a complete reference for this relatively new, but increasingly important area of molecular spectroscopy. Key features: A single-source reference on this topic that introduces, describes the background and foundation of this area of spectroscopy. Serves as a guide on how to use it to carry out applications with relevant problem solving. Depth and breadth of the subject is presented in a logical, complete and progressive fashion. Although intended as an introductory text, this book provides in depth coverage of this topic relevant to both students and professionals by taking the reader from basic theory through to practical and instrumental approaches.