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About this product
- Author(s)Mark W. Holladay,Richard B. Silverman
- PublisherElsevier Science Publishing Co Inc
- Date of Publication21/05/2014
- GenreIndustrial Chemistry & Manufacturing
- Place of PublicationSan Diego
- Country of PublicationUnited States
- ImprintAcademic Press Inc
- Weight1720 g
- Edition Statement3rd edition
- Table Of Contents1. Introduction 1.1. Overview 1.2. Drugs Discovered without Rational Design 1.2.1. Medicinal Chemistry Folklore 1.2.2. Discovery of Penicillins 1.2.3. Discovery of Librium 1.2.4. Discovery of Drugs through Metabolism Studies 1.2.5. Discovery of Drugs through Clinical Observations 1.3. Overview of Modern Rational Drug Design 1.3.1. Overview of Drug Targets 1.3.2. Identification and Validation of Targets for Drug Discovery 1.3.3. Alternatives to Target-Based Drug Discovery 1.3.4. Lead Discovery 1.3.5. Lead Modification (Lead Optimization) 22.214.171.124. Potency 126.96.36.199. Selectivity 188.8.131.52. Absorption, Distribution, Metabolism, and Excretion (ADME) 184.108.40.206. Intellectual Property Position 1.3.6. Drug Development 220.127.116.11. Preclinical Development 18.104.22.168. Clinical Development (Human Clinical Trials) 22.214.171.124. Regulatory Approval to Market the Drug 1.4. Epilogue 1.5. General References 1.6. Problems References 2. Lead Discovery and Lead Modification 2.1. Lead Discovery 2.1.1. General Considerations 2.1.2. Sources of Lead Compounds 126.96.36.199. Endogenous Ligands 188.8.131.52. Other Known Ligands 184.108.40.206. Screening of Compounds 220.127.116.11.1. Sources of Compounds for Screening 18.104.22.168.1.1. Natural Products 22.214.171.124.1.2. Medicinal Chemistry Collections and Other Handcrafted Compounds 126.96.36.199.1.3. High-Throughput Organic Synthesis 188.8.131.52.1.3.1. Solid-Phase Library Synthesis 184.108.40.206.1.3.2. Solution-Phase Library Synthesis 220.127.116.11.1.3.3. Evolution of HTOS 18.104.22.168.2. Drug-Like, Lead-Like, and Other Desirable Properties of Compounds for Screening 22.214.171.124.3. Random Screening 126.96.36.199.4. Targeted (or Focused) Screening, Virtual Screening, and Computational Methods in Lead Discovery 188.8.131.52.4.1. Virtual Screening Database 184.108.40.206.4.2. Virtual Screening Hypothesis 220.127.116.11.5. Hit-To-Lead Process 18.104.22.168.6. Fragment-based Lead Discovery 2.2. Lead Modification 2.2.1. Identification of the Active Part: The Pharmacophore 2.2.2. Functional Group Modification 2.2.3. Structure-Activity Relationships 2.2.4. Structure Modifications to Increase Potency, Therapeutic Index, and ADME Properties 22.214.171.124. Homologation 126.96.36.199. Chain Branching 188.8.131.52. Bioisosterism 184.108.40.206. Conformational Constraints and Ring-Chain Transformations 220.127.116.11. Peptidomimetics 2.2.5. Structure Modifications to Increase Oral Bioavailability and Membrane Permeability 18.104.22.168. Electronic Effects: The Hammett Equation 22.214.171.124. Lipophilicity Effects 126.96.36.199.1. Importance of Lipophilicity 188.8.131.52.2. Measurement of Lipophilicities 184.108.40.206.3. Computer Automation of log P Determination 220.127.116.11.4. Membrane Lipophilicity 18.104.22.168. Balancing Potency of Ionizable Compounds with Lipophilicity and Oral Bioavailability 22.214.171.124. Properties that Influence Ability to Cross the Blood-Brain Barrier 126.96.36.199. Correlation of Lipophilicity with Promiscuity and Toxicity 2.2.6. Computational Methods in Lead Modification 188.8.131.52. Overview 184.108.40.206. Quantitative Structure-Activity Relationships (QSARs) 220.127.116.11.1. Historical Overview. Steric Effects: The Taft Equation and Other Equations 18.104.22.168.2. Methods Used to Correlate Physicochemical Parameters with Biological Activity 22.214.171.124.2.1. Hansch Analysis: A Linear Multiple Regression Analysis 126.96.36.199.2.2. Manual Stepwise Methods: Topliss Operational Schemes and Others
- Author BiographyProfessor Richard B. Silverman received his B.S. degree in chemistry from The Pennsylvania State University in 1968 and his Ph.D. degree in organic chemistry from Harvard University in 1974 (with time off for a two-year military obligation from 1969-1971). After two years as a NIH postdoctoral fellow in the laboratory of the late Professor Robert Abeles in the Graduate Department of Biochemistry at Brandeis University, he joined the chemistry faculty at Northwestern University. In 1986, he became Professor of Chemistry and Professor of Biochemistry, Molecular Biology, and Cell Biology. In 2001, he became the Charles Deering McCormick Professor of Teaching Excellence for three years, and since 2004 he has been the John Evans Professor of Chemistry. His research can be summarized as investigations of the molecular mechanisms of action, rational design, and syntheses of potential medicinal agents acting on enzymes and receptors. His awards include DuPont Young Faculty Fellow (1976), Alfred P. Sloan Research Fellow (1981-1985), NIH Research Career Development Award (1982-1987), Fellow of the American Institute of Chemists (1985), Fellow of the American Association for the Advancement of Science (1990), Arthur C. Cope Senior Scholar Award of the American Chemical Society (2003), Alumni Fellow Award from Pennsylvania State University (2008), Medicinal Chemistry Hall of Fame of the American Chemical Society (2009), the Perkin Medal from the Society of Chemical Industry (2009), the Hall of Fame of Central High School of Philadelphia (2011), the E.B. Hershberg Award for Important Discoveries in Medicinally Active Substances from the American Chemical Society (2011), Fellow of the American Chemical Society (2011), Sato Memorial International Award of the Pharmaceutical Society of Japan (2012), Roland T. Lakey Award of Wayne State University (2013), BMS-Edward E. Smissman Award of the American Chemical Society (2013), the Centenary Prize of the Royal Society of Chemistry (2013), and the Excellence in Medicinal Chemistry Prize of the Israel Chemical Society (2014). Professor Silverman has published over 320 research and review articles, holds 49 domestic and foreign patents, and has written four books (The Organic Chemistry of Drug Design and Drug Action is translated into German and Chinese). He is the inventor of LyricaTM, a drug marketed by Pfizer for epilepsy, neuropathic pain, fibromyalgia, and spinal cord injury pain; currently, he has another CNS drug in clinical trials. Dr. Mark W. Holladay is Vice President of Drug Discovery and Medicinal Chemistry at Ambit Biosciences (San Diego, California) where he leads drug discovery programs in oncology and autoimmune diseases and has contributed to compounds in clinical development. He began his drug hunting career at Abbott Laboratories where he achieved the position of Volwiler Associate Research Fellow as a medicinal chemist and project leader in the Neurosciences Research Area. He also conducted collaborative drug discovery research as a member of contract research organizations including Biofocus and Discovery Partners International. He is a co-author on over 70 peer-reviewed research articles, reviews, or chapters and is named as an inventor on over 40 patents and patent applications. Dr. Holladay earned his undergraduate degree from Vanderbilt University, his Ph.D. at Northwestern University under the direction of Professor Richard B. Silverman, and conducted postdoctoral studies with Professor Daniel H. Rich at the University of Wisconsin-Madison.
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