The Practice of Medicinal Chemistry

by Camille Georges Wermuth (Editor)

Overview

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.

• 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

Product Details

ISBN-13:	9780080497778
Publisher:	Elsevier Science
Publication date:	06/11/2003
Sold by:	Barnes & Noble
Format:	eBook
Pages:	736
File size:	25 MB
Note:	This product may take a few minutes to download.

About the Author

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.

Table of Contents

Drug Targets
Natural Products
Electronic Screening
Identical and Non-Identical Twin Drugs
Optical Isomerism in Drugs and more

What People are Saying About This

From the Publisher

A complete guide to the drug discovery process for medicinal chemists

Editorial Reviews

3 Stars from Doody

Reviewer: Lester A Mitscher, Ph. D.(Kansas University)
Description: This is an advanced introductory treatment of medicinal chemistry for practitioners in the field, especially those who are within five years of their first professional and postgraduate appointment in a discovery environment. It is not a text for undergraduate students whose primary interest is in distributive medicine. It is organized according to discovery techniques rather than a disease orientation. The first edition was published in 1996 and was well received.
Purpose: The book is intended primarily for organic chemists beginning a career in drug research and as a source for academic and industrial medicinal chemists. The book emphasizes techniques for optimization of leads discovered in screening programs. This edition is revised to include important discoveries made in the nine years since the appearance of the first edition. This is a worthy objective that the book meets quite well.
Audience: The book is written primarily for organic chemists familiar with synthesis but weak in biological applications. Particularly, it is intended for those in their early years as practitioners of medicinal chemistry. Pharmacologists, biochemists and other life scientists who have an interest in drug design, development, and optimization can also profit from reading this work. These are the editor's objectives and they are in line with my sense of the needs of many scientists. The editor has been an influential scientist in academic and now industrial medicinal chemistry and has recruited an outstanding cadre of chapter authors well versed in the field and practicing in the major drug markets on three continents.
Features: This second edition has the same intent as the first and follows much the same format with many of the same authors and many of the same chapter headings. The chapters have been revised and brought up-to-date and several have been totally rewritten. This edition is physically about the same thickness but the pages are larger, so even though it has 768 pages compared with the 968 pages of the first edition, it now has a double column format so the contents have not been reduced in order to decrease the length. As before, the book is divided into eight parts and runs to 43 chapters, eight of which have new titles and four have new authors. These chapters are mostly significantly improved over the previous versions. Those that have the same titles and same authors have been rewritten, often extensively. Particularly notable are the outstanding treatments of natural products chemistry by David Newman, Gordon Cragg and David Kingston; the discussion of homologous series and of bioisosteres by Camille Wermuth; the role of functional groups in drug receptor interactions by Peter Andrews; compound properties and drug qualities by Christopher Lipinski; Stereochemical aspects by Daniel Rich; agonist to antagonist conversions by David Triggle and legal aspects of product protection by Maria Souleau. The book succeeds remarkably well in presenting a reasonably balanced overview of the field in a single book. The reader's appetite for more material is whetted but not sated. Those needing a more advanced treatment will need to refer to Comprehensive Medicinal Chemistry: General Principles (Pergamon Press, 1991) or to the most recent revision of Burger's Medicinal Chemistry and Drug Discovery (John Wiley & Sons, 2003).
Assessment: 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 Review Service

A useful, authoritative discussion of the principles and practice of medicinal chemistry... the volume has a useful index, is well produced and is very reasonably priced." — JOURNAL OF MEDICINAL CHEMISTRY

From the Publisher