Bibliothèque de L'IMIST/CNRST

Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists with little or no background in medicinal chemistry. These chemists must acquire a good knowledge of medicinal chemistry during their first years in the pharmaceutical/drug discovery industry. This book aims to be their practical handbook - a complete guide to the drug discovery process. The book reviews practical aspects of Medicinal Chemistry, emphasising the daily problems met by the medicinal chemist when dealing with lead discovery/identification methodologies, with structure-activity relationship studies aimed to scale up potency and target selectivity, and when optimising pharmacokinetic and pharmaceutical properties by means of ultimate chemical modifications. This is the second edition of The Practice of Medicinal Chemistry, the first edition being published in February 1996. The new edition is thoroughly revised, with around 30% new material, and refocussed to reflect the recent developments in genomics, proteomics, high throughput screening of compounds and drug solubilisation. An effort has been made to remove the overlap that exists in the previous edition and four new chapters have been introduced. * Written by experts in the field * The first edition of The Practice of Medicinal Chemistry, published in 1996, was nicknamed 'The Bible' by medicinal chemists. * The only available book dealing with the practical aspects of medicinal chemistry, from conception of the molecules through to the production of drugs * An essential practical handbook for the medicinal chemist, working in the pharmaceutical industry, with little or no background in medicinal chemistry-a complete guide to the drug discovery process.

Foreward. -- Preface. -- A Brief History Of Drugs -- From Plant Extracts To DNA Technology -- Medicinal Chemistry: Definition And Objectives, The Three Main Phases Of Drug Activity, Drug And Diseases Classifications -- Measurement And Expression Of Drug Effects -- Drug Targets: Molecular Mechanisms Of Drug Action -- Strategies In The Search For New Lead Compounds Or Original Working Hypotheses -- Natural Products As Pharmaceuticals And Sources For Lead Structures -- Basics Of Combinatorial Chemistry -- The Contribution Of Molecular Biology To Drug Discovery -- Electronic Screening: Lead Finding From Database Mining -- High-Speed Chemistry Libraries: Assessment Of Drug-Likeness -- Web Alert Using The Internet For Medicinal Chemistry -- Molecular Variations In Homologous Series: Vinylogues And Benzologues -- Molecular Variations Based On Isosteric Replacements -- Ring Transformations -- Introduction Of Conformational Restriction And/Or Steric Hindrance -- Identical And Non Identical Twin Drugs -- Optical Isomerism In Drugs -- Application Strategies For The Primary Structure-Activity Relationship Exploration -- Specific Substituent Groups -- The Role Of Functional Groups In Drug-Receptor Interactions -- Compound Properties And Drug Quality -- Quantitative Approaches To Structure-Activity Relationships -- Structural Aspects Of Drug Action I -- Pharmacophore Identification And Receptor Mapping -- Three-Dimentional Quantitative Structure-Property Relationships -- Protein Crystallography And Drug Discovery -- Protein Comparative Modelling And Drug Discovery -- The Transition From Agonist To Antagonist Activity: Symmetry And Other Considerations -- Design Of Peptidomimetics -- The Fate Of Xenobiotics In Living Organisms -- Biotransformation Reactions -- Chemical Mechanisms Of Toxicity -- Basic Knowledge For Designing Safer Drugs -- Designing Prodrugs And Bioprecursors -- Macromolecular Carriers For Drug Targeting -- Preparation Of Water Soluble Compounds Through Salt Formation -- Preparation Of Water-Soluble Compounds By Covalent Attachment Of Solubilizing Moieties -- Drug Solubilization With Organic Solvents, Surfactants And Lipids -- Improvement Of Drug Properties By Cyclodextrins -- Chemical And Physicochemical Solutions To Formulation Problems -- Discover A Drug Substance, Formulate And Develop It To A Product -- Drug Nomenclature -- Legal Aspects Of Product Protection -- The Consumption And Production Of Pharmaceuticals.

Includes bibliographical references and index.

Description based on print version record.