The Practice of Medicinal Chemistry - 2nd Edition - ISBN: 9780127444819, 9780080497778

The Practice of Medicinal Chemistry

2nd Edition

Editors: Camille Wermuth Camille Wermuth
Hardcover ISBN: 9780127444819
eBook ISBN: 9780080497778
Imprint: Academic Press
Published Date: 11th June 2003
Page Count: 736
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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

Details

No. of pages:
736
Language:
English
Copyright:
© Academic Press 2003
Published:
11th June 2003
Imprint:
Academic Press
Hardcover ISBN:
9780127444819
eBook ISBN:
9780080497778

About the Editor

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

Reviews

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

Ratings and Reviews