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Informationen zum Autor NICHOLAS BODOR is Graduate Research Professor Emeritus (active) at the University of Florida. He has over 500 publications and 220 patents to his credit. His many awards include the Florida Scientist of the Year, the Volweiler Award, the Distinguished Pharmaceutical Scientist Award, the Fabinyi Prize, and the Commander's Cross of the Order of Merit of Hungary. He holds numerous honorary doctor degrees. He was elected to the Hungarian Academy of Sciences and inducted to the ACS Medicinal Chemistry Hall of Fame. PETER BUCHWALD is Assistant Professor in the Department of Molecular and Cellular Pharmacology and Director of Drug Discovery for the Diabetes Research Institute at the University of Miami. He is the author of nine book chapters and eighty-six peer-reviewed publications. Klappentext Innovative approach to drug design that's more likely to result in an approvable drug productRetrometabolic drug design incorporates two distinct drug design approaches to obtain soft drugs and chemical delivery systems, respectively. Combining fundamentals with practical step-by-step examples, Retrometabolic Drug Design and Targeting gives readers the tools they need to take full advantage of retrometabolic approaches in order to develop safe and effective targeted drug therapies. The authors, both pioneers in the fields of soft drugs and retrometabolic drug design, offer valuable ideas, approaches, and solutions to a broad range of challenges in drug design, optimization, stability, side effects, and toxicity.Retrometabolic Drug Design and Targeting begins with an introductory chapter that explores new drugs and medical progress as well as the challenges of today's drug discovery. Next, it discusses:* Basic concepts of the mechanisms of drug action* Drug discovery and development processes* Retrometabolic drug design* Soft drugs* Chemical delivery systemsInside the book, readers will find examples from different pharmacological areas detailing the rationale for each drug design. These examples set forth the relevant pharmacokinetic and pharmacodynamic properties of the new therapeutic agents, comparing these properties to those of other compounds used for the same therapeutic purpose. In addition, the authors review dedicated computer programs that are available to support and streamline retrometabolic drug design efforts.Retrometabolic Drug Design and Targeting is recommended for all drug researchers interested in employing this newly tested and proven approach to developing safe and effective drugs. Zusammenfassung Innovative approach to drug design that's more likely to result in an approvable drug product Retrometabolic drug design incorporates two distinct drug design approaches to obtain soft drugs and chemical delivery systems, respectively. Inhaltsverzeichnis Preface ix 1 Introduction 1 1.1 New Drugs and Medical Progress 1 1.2 The Challenge of New Drug Discovery 5 References 7 2 Mechanism of Drug Action: Basic Concepts 9 2.1 Pharmacodynamic Phase: Drug-Receptor Interactions 10 2.1.1 The Receptor Concept and Receptor Types 10 2.1.2 Ligand-Receptor Binding 12 2.1.3 Receptor Occupancy and Activation 16 2.2 Pharmacokinetic Phase: ADME 20 2.2.1 Drug Absorption and Distribution 20 2.2.2 Drug Metabolism and Excretion 22 2.2.3 Basic Pharmacokinetic Concepts 26 2.3 Structural Requirements: Keeping It "Drug-Like" 29 2.3.1 The Drug-Like Chemical Space 29 2.3.2 Oral Drugs: The Challenge of Bioavailability 31 References 33 3 The Drug Discovery and Development Process 39 3.1 Discovery Research 39 3.1.1 Prediscovery 39 3.1.2 Target Identification 41 3.1.3 Target Validation 42 3.1.4 Target-to-Hit and Hit-to-Lead Development 42 3.1.5 Early Distribution and Safet...
