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The Practice of Medicinal Chemistry (Third Edition)
By Camille Wermuth, Prestwick Chemical, Illkirch, France
Publisher: Academic Press
Number Of Pages: 982
Publication Date: 2008-07-23
ISBN-10 / ASIN: 0123741947
ISBN-13 / EAN: 9780123741943
Binding: Hardcover
Description
Now in its third edition, this classic reference is the one-stop-shop for information on the foundations of medicinal chemistry for pharmaceutical researchers who are involved in drug development & discovery but who do not have a background in medicinal chemistry. Wermuth aids pharmaceutical researchers and chemists in making faster, more accurate identifications of the active substances that could potentially treat the disorder they are researching. New chapters on Drug Absorption & Transport give pharmaceutical scientists information on how potential drugs can move through the drug discovery/development phases more quickly. This third edition still stands as the only source for practical aspects of medicinal chemistry by focusing on the daily problems met by the medicinal chemist in drug discovery.
Audience
Pharmaceutical researchers in drug discovery, chemists
Table of Contents
Biography, Pages xxv-xxvi
Contributors, Pages xxix-xxxiii
Preface to the First Edition, Pages xxxv-xxxvi
Preface to the Second Edition, Pages xxxvii-xxxviii
Preface to the Third Edition, Page xxxix
Part I: General Aspects of Medicinal Chemistry
Chapter 1 - A History of Drug DiscoveryFrom first steps of chemistry to achievements in molecular pharmacology, Pages 1-62, François Chast
Chapter 2 - Medicinal ChemistryDefinitions and Objectives, Drug Activity Phases, Drug Classification Systems, Pages 63-72, Peter Imming
Chapter 3 - Measurement and Expression of Drug Effects, Pages 73-84, Jean-Pierre Nowicki, Bernard Scatton
Chapter 4 - Molecular Drug Targets, Pages 85-105, Jean-Pierre Gies, Yves Landry
Chapter 5 - Drug Targets, Target identification, Validation and Screening, Pages 106-121, Kenton H. Zavitz, Paul L. Bartel, Adrian N. Hobden
Part II: Lead Compound Discovery Strategies
Chapter 6 - Strategies in the Search for New Lead Compounds or Original Working Hypotheses, Pages 123-143, Camille G. Wermuth
Chapter 7 - High-Throughput Screening and Drug Discovery, Pages 144-158, John R. Proudfoot
Chapter 8 - Natural Products as Pharmaceuticals and Sources for Lead Structures, Pages 159-186, David J. Newman, Gordon M. Cragg, David G. I. Kingston
Chapter 9 - Biology Oriented Synthesis and Diversity Oriented Synthesis in Compound Collection Development, Pages 187-209, Kamal Kumar, Stefan Wetzel, Herbert Waldmann
Chapter 10 - In Silico ScreeningHit Finding from Database Mining, Pages 210-227, Thierry Langer, Sharon D. Bryant
Chapter 11 - Fragment-Based Drug Discovery, Pages 228-243, Bennett T. Farmer, Allen B. Reitz
Chapter 12 - Lead-Likeness and Drug-Likeness, Pages 244-254, Alex Polinsky
Chapter 13 - Web AlertUsing the Internet for Medicinal Chemistry, Pages 255-272, David Cavalla
Part III: Primary Exploration of Structure–Activity Relationships
Chapter 14 - Molecular Variations in Homologous SeriesVinylogues and Benzologues, Pages 273-289, Camille G. Wermuth
Chapter 15 - Molecular Variations Based on Isosteric Replacements, Pages 290-342, Paola Ciapetti, Bruno Giethlen
Chapter 16 - Ring Transformations, Pages 343-362, Christophe Morice, Camille G. Wermuth
Chapter 17 - Conformational Restriction and/or Steric Hindrance in Medicinal Chemistry, Pages 363-379, André Mann
Chapter 18 - Homo and Heterodimer Ligands: the Twin Drug Approach, Pages 380-414, Jean-Marie Contreras, Wolfgang Sippl
Chapter 19 - Application Strategies for the Primary Structure–Activity Relationship Exploration, Pages 415-427, Camille G. Wermuth
Part IV: Substituents and Functions: Qualitative and Quantitative Aspects of Structure–Activity Relationships
Chapter 20 - Substituent Groups, Pages 429-463, Patrick Bazzini, Camille G. Wermuth
Chapter 21 - The Role of Functional Groups in Drug–Receptor Interactions, Pages 464-480, Laurent Schaeffer
Chapter 22 - Compound Properties and Drug Quality, Pages 481-490, Christopher A. Lipinski
Chapter 23 - Quantitative Approaches to Structure–Activity Relationships, Pages 491-513, Han van de Waterbeemd, Sally Rose
Part V: Spatial Organization, Receptor Mapping and Molecular Modeling
Chapter 24 - OverviewThe Search for Biologically Useful Chemical Space, Pages 515-520, David J. Triggle
Chapter 25 - Pharmacological Space, Pages 521-532, Andrew L. Hopkins
Chapter 26 - Optical Isomerism in Drugs, Pages 533-548, Camille G. Wermuth
Chapter 27 - Multi-target DrugsStrategies and Challenges for Medicinal Chemists, Pages 549-571, Richard Morphy, Zoran Rankovic
Chapter 28 - Pharmacophore Identification and Pseudo-Receptor Modeling, Pages 572-586, Wolfgang Sippl
Chapter 29 - 3D Quantitative Structure–Property Relationships, Pages 587-604, Thierry Langer, Sharon D. Bryant
Chapter 30 - Protein Crystallography and Drug Discovery, Pages 605-634, Jean-Michel Rondeau, Herman Schreuder
Part VI: Chemical Modifications Infl uencing the Pharmacokinetic Properties
Chapter 31 - Physiological Aspects Determining the Pharmacokinetic Properties of Drugs, Pages 635-654, Koen Boussery, Frans M. Belpaire, Johan Van de Voorde
Chapter 32 - Biotransformation Reactions and Their Enzymes, Pages 655-673, Bernard Testa
Chapter 33 - Biotransformations Leading to Toxic MetabolitesChemical Aspect, Pages 674-696, Anne-Christine Macherey, Patrick M. Dansette
Chapter 34 - Drug Transport Mechanisms and their Impact on the Disposition and Effects of Drugs, Pages 697-710, Jean-Michel Scherrmann
Chapter 35 - Strategies for Enhancing Oral Bioavailability and Brain Penetration, Pages 711-720, Brian C. Shook, Paul F. Jackson
Chapter 36 - Designing Prodrugs and Bioprecursors, Pages 721-746, Camille G. Wermuth
Part VII: Pharmaceutical and Chemical Means to Solubility and Formulation Problems
Chapter 37 - Preparation of Water-Soluble Compounds Through Salt Formation, Pages 747-766, Michael J. Bowker, P. Heinrich Stahl
Chapter 38 - Preparation of Water-Soluble Compounds by Covalent Attachment of Solubilizing Moieties, Pages 767-785, Camille G. Wermuth
Chapter 39 - Drug Solubilization with Organic Solvents, or Using Micellar Solutions or Other Colloidal Dispersed Systems, Pages 786-812, Michael J. Bowker, P. Heinrich Stahl
Chapter 40 - Improvement of Drug Properties by Cyclodextrins, Pages 813-840, Kaneto Uekama, Fumitoshi Hirayama
Chapter 41 - Chemical and Physicochemical Approaches to Solve Formulation Problems, Pages 841-853, Camille G. Wermuth
Part VIII: Development of New Drugs: Legal and Economic Aspects
Chapter 42 - Discover a Drug Substance, Formulate and Develop It to a Product, Pages 855-866, Bruno Galli, Bernard Faller
Chapter 43 - Drug Nomenclature, Pages 867-877, R.G. Balocco Mattavelli, J.C. Dong, S. Lasseur, S. Kopp
Chapter 44 - Legal Aspects of Product ProtectionWhat a Medicinal Chemist Should Know About Patent Protection, Pages 878-893, Maria Souleau
Chapter 45 - The Consumption and Production of Pharmaceuticals, Pages 894-921, Bryan G. Reuben
Index, Pages 923-942
http://www.elsevier.com/wps/find ... ription#description
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