The Practice of Medicinal Chemistry
Edited by- Camille Wermuth, Prestwick Chemical, Illkirch, France
- Camille Wermuth, Prestwick Chemical, Illkirch, France
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.
Audience
Academic and industrial organic chemists/pharmacologists beginning a career in drug research, established scientists teaching medicinal chemistry, graduate and post-graduate medicinal chemists, biochemists, physical chemists, structural biologists, protein chemists, molecular biologists, and researchers and scientists in the pharmaceutical industry.
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Published: June 2003
Imprint: Academic Press
ISBN: 978-0-12-744481-9
Reviews
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"...it is a practical guide with many examples from the recent literature...it serves as an excellent introduction to those just starting a career in medicinal chemistry...Because these chapters are organized as reviews, they will serve as a good resource for those already working as medicinal chemists. The chapter on natural products provides an interesting analysis of marketed drugs and compounds in the clinic that supports their use as an important source of leads. In summary, this is a book that should be included in the libraries of companies and institutions where medicinal chemistry in practiced." -John W. Ellingboe, Wyeth Research, New York "The Practice of Medicinal Chemistry is highly recommended for medical libraries and academic libraries that support a chemistry program." -E-STREAMS (May 2004) "Practicing medicinal chemists, particularly those within five years of their first post-school appointment in the area, will profit from buying and studying this book. Pharmacologists and others interacting with medicinal chemists will also find this book to be useful in their professional work. Those who liked the first edition will like this one even better." -DOODY'S (March 2004) "...capture[s] the whole spectrum of activities associated with both the theory and practice of rational drug design. ...an impressive book suitable for not only Medicinal Chemists of all experience levels but for anyone working in the field of drug discovery. It would be a welcome addition to any drug discoverer's book shelf." -BRITISH JOURNAL OF CLINICAL PHARMACOLOGY (2003) PRAISE FOR THE FIRST EDITION "...a useful, authoritative discussion of the principles and practice of medicinal chemistry...the volume has a useful index, is well produced, and is very resonably priced..." -JOURNAL OF MEDICINAL CHEMISTRY
Contents
- Foreward.Preface.A Brief History Of DrugsFrom Plant Extracts To DNA TechnologyMedicinal Chemistry: Definition And Objectives, The Three Main Phases Of Drug Activity, Drug And Diseases ClassificationsMeasurement And Expression Of Drug EffectsDrug Targets: Molecular Mechanisms Of Drug ActionStrategies In The Search For New Lead Compounds Or Original Working HypothesesNatural Products As Pharmaceuticals And Sources For Lead StructuresBasics Of Combinatorial ChemistryThe Contribution Of Molecular Biology To Drug DiscoveryElectronic Screening: Lead Finding From Database MiningHigh-Speed Chemistry Libraries: Assessment Of Drug-LikenessWeb Alert Using The Internet For Medicinal ChemistryMolecular Variations In Homologous Series: Vinylogues And BenzologuesMolecular Variations Based On Isosteric ReplacementsRing TransformationsIntroduction Of Conformational Restriction And/Or Steric HindranceIdentical And Non Identical Twin DrugsOptical Isomerism In DrugsApplication Strategies For The Primary Structure-Activity Relationship ExplorationSpecific Substituent GroupsThe Role Of Functional Groups In Drug-Receptor InteractionsCompound Properties And Drug QualityQuantitative Approaches To Structure-Activity RelationshipsStructural Aspects Of Drug Action IPharmacophore Identification And Receptor MappingThree-Dimentional Quantitative Structure-Property RelationshipsProtein Crystallography And Drug DiscoveryProtein Comparative Modelling And Drug DiscoveryThe Transition From Agonist To Antagonist Activity: Symmetry And Other ConsiderationsDesign Of PeptidomimeticsThe Fate Of Xenobiotics In Living OrganismsBiotransformation ReactionsChemical Mechanisms Of ToxicityBasic Knowledge For Designing Safer DrugsDesigning Prodrugs And Bioprecursors Macromolecular Carriers For Drug TargetingPreparation Of Water Soluble Compounds Through Salt FormationPreparation Of Water-Soluble Compounds By Covalent Attachment Of Solubilizing MoietiesDrug Solubilization With Organic Solvents, Surfactants And LipidsImprovement Of Drug Properties By CyclodextrinsChemical And Physicochemical Solutions To Formulation ProblemsDiscover A Drug Substance, Formulate And Develop It To A ProductDrug NomenclatureLegal Aspects Of Product ProtectionThe Consumption And Production Of Pharmaceuticals
