The Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry

2nd Edition - June 11, 2003

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  • Editors: Camille Wermuth, Camille Wermuth
  • eBook ISBN: 9780080497778

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Description

The Practice of Medicinal Chemistry, 2E, is a single-volume source on the practical aspects of medicinal chemistry. The successful first edition was nicknamed "The Bible" by medicinal chemists, and the second edition has been updated, expanded and refocused to reflect developments over the last decade. Emphasis is put on how medicinal chemists conduct their search for and design of new drug entities. In contrast to competing books, it focuses on the chemistry rather than pharmacological concepts or descriptions of the various therapeutic classes of drugs. Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists who must acquire a strong knowledge of medicinal chemistry as they enter the industry. This book aims to be their practical handbook - a complete guide to the drug discovery process.

Key Features

  • The only book available dealing with the practical aspects of medicinal chemistry
  • Serves as a complete guide to the drug discovery process, from conception of the molecules to drug production
  • Updated chapters devoted to the discovery of new lead compounds, including combinatorial chemistry

Readership

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

Table of Contents

  • 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

Product details

  • No. of pages: 736
  • Language: English
  • Copyright: © Academic Press 2003
  • Published: June 11, 2003
  • Imprint: Academic Press
  • eBook ISBN: 9780080497778

About the Editors

Camille Wermuth

Camille Wermuth

Camille-Georges Wermuth PhD, Prof. and Founder of Prestwick Chemical, was Professor of Organic Chemistry and Medicinal Chemistry at the Faculty of Pharmacy, Louis Pasteur University, Strasbourg, France from 1969 to 2002. He became interested in Medicinal Chemistry during his two years of military service in the French Navy at the "Centre d’Etudes Physio-biologiques Appliquées à la Marine" in Toulon. During this time he worked under the supervision of Dr Henri Laborit, the scientist who invented artificial hibernation and discovered chlorpromazine.

Professor Wermuths’ main research themes focus on the chemistry and the pharmacology of pyridazine derivatives. The 3-aminopyridazine pharmacophore, in particular, allowed him to accede to an impressive variety of biological activities, including antidepressant and anticonvulsant molecules; inhibitors of enzymes such as mono-amine-oxidases, phosphodiesterases and acetylcholinesterase; ligands for neuro-receptors: GABA-A receptor antagonists, serotonine 5-HT3 receptor antagonists, dopaminergic and muscarinic agonists. More recently, in collaboration with the scientists of the Sanofi Company, he developed potent antagonists of the 41 amino-acid neuropeptide CRF (corticotrophin-releasing factor) which regulates the release of ACTH and thus the synthesis of corticoids in the adrenal glands. Professor Wermuth has also, in collaboration with Professor Jean-Charles Schwartz and Doctor Pierre Sokoloff (INSERM, Paris), developed selective ligands of the newly discovered dopamine D3 receptor. After a three-year exploratory phase, this research has led to nanomolar partial agonists which may prove useful in the treatment of the cocaine-withdrawal syndrome.

Dr. Wermuth is co-author or editor of several books, the author of over 250 scientific papers and holds nearly 60 patents. Professor Wermuth is also the recipient of the Charles Mentzer Prize of the Société Française de Chimie Thérapeutique, the Léon Velluz Prize of the French Academy of Science, the Prix de l'Ordre des Pharmaciens by the French Academy of Pharmacy and the Nauta Award of the European Federation for Medicinal Chemistry for Pharmacochemistry in 2010.

Affiliations and Expertise

Prestwick Chemical, Illkirch, France

Camille Wermuth

Camille Wermuth

Camille-Georges Wermuth PhD, Prof. and Founder of Prestwick Chemical, was Professor of Organic Chemistry and Medicinal Chemistry at the Faculty of Pharmacy, Louis Pasteur University, Strasbourg, France from 1969 to 2002. He became interested in Medicinal Chemistry during his two years of military service in the French Navy at the "Centre d’Etudes Physio-biologiques Appliquées à la Marine" in Toulon. During this time he worked under the supervision of Dr Henri Laborit, the scientist who invented artificial hibernation and discovered chlorpromazine.

Professor Wermuths’ main research themes focus on the chemistry and the pharmacology of pyridazine derivatives. The 3-aminopyridazine pharmacophore, in particular, allowed him to accede to an impressive variety of biological activities, including antidepressant and anticonvulsant molecules; inhibitors of enzymes such as mono-amine-oxidases, phosphodiesterases and acetylcholinesterase; ligands for neuro-receptors: GABA-A receptor antagonists, serotonine 5-HT3 receptor antagonists, dopaminergic and muscarinic agonists. More recently, in collaboration with the scientists of the Sanofi Company, he developed potent antagonists of the 41 amino-acid neuropeptide CRF (corticotrophin-releasing factor) which regulates the release of ACTH and thus the synthesis of corticoids in the adrenal glands. Professor Wermuth has also, in collaboration with Professor Jean-Charles Schwartz and Doctor Pierre Sokoloff (INSERM, Paris), developed selective ligands of the newly discovered dopamine D3 receptor. After a three-year exploratory phase, this research has led to nanomolar partial agonists which may prove useful in the treatment of the cocaine-withdrawal syndrome.

Dr. Wermuth is co-author or editor of several books, the author of over 250 scientific papers and holds nearly 60 patents. Professor Wermuth is also the recipient of the Charles Mentzer Prize of the Société Française de Chimie Thérapeutique, the Léon Velluz Prize of the French Academy of Science, the Prix de l'Ordre des Pharmaciens by the French Academy of Pharmacy and the Nauta Award of the European Federation for Medicinal Chemistry for Pharmacochemistry in 2010.

Affiliations and Expertise

Prestwick Chemical, Illkirch, France

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