The Practice of Medicinal Chemistry,

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9780127444819: The Practice of Medicinal Chemistry,

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 per cent 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. It is 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. It is the only available book dealing with the practical aspects of medicinal chemistry, from conception of the molecules through to the production of drugs. It is an essential practical handbook for the medicinal chemist, working in the pharmaceutical industry, with little or no background in medicinal chemistry.

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Review:

"...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

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 Appliquees a 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. Besides about 300 scientific papers and about 60 patents, Professor Wermuth is co-author or editor of several books including; Pharmacologie Moleculaire, Masson & Cie, Paris; Medicaments Organiques de Synthese, Masson & Cie, Paris; Medicinal Chemistry for the 21st Century, Bl

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