The Practice of Medicinal Chemistry

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9780127446400: The Practice of Medicinal Chemistry

This book collects in one single volume, the practical aspects of Medicinal Chemistry, seen from a chemical point of view, including the wealth of information which chemists accumulate over a career, but generally is never organized and presented in a coherent form in print. Emphasis is given to how medicinal chemists conduct their search for, and design of, new drug entities. In contrast to other books on the market, it focuses on the chemistry, rather than pharmacological concepts or description of the various therapeutic classes of drugs. It should become a standard reference on the tools available to medicinal chemists when designing new drugs.

Key Features
* These aspects are covered by:
* Specific chapters devoted to the discovery of new lead compounds, including combinatorial chemistry
* Clearly written chapters on modern topics such as stereochemical aspects of drug action, the use of X-ray structures of receptors and enzymes in drug discovery, and the contribution of molecular biology to drug discovery
* Guidelines and operational strategems allowing identification of the portions of the molecule which are important for potency
* The particular emphasis given to the three-dimensional aspects of the drug-receptor interactions, to the design of peptidomimetic drugs and to the control of the agonist-antagonist transition
* Chemical solutions to solubility and to formulation problems These sections cover perhaps the most neglected areas in medicinal chemistry books
* Development of new drugs: legal and economic aspects, constitutes another important area in which chemists are almost wholly self taught following their entry into industry

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From the Back Cover:

This book collects in one single volume the practical aspects of Medicinal Chemistry, seen from the chemical point of view, including the wealth of information which medicinal chemists accumulate over a career, and is generally never organized and presented in coherent form in print. Emphasis is given to the daily problems met by the medicinal chemist when he deals with lead discovery and identification methodologies, with structure-activity relationship studies aimed to scale up potency and target selectivity, and when he has to confer optimal pharmaceutic properties by means of ultimate chemical modifications.
These aspects are covered by:
* Specific chapters devoted to the discovery of new lead compounds, including combinatorial chemistry.
* Clearly written chapters on modern topics such as stereochemical aspects of drug action, the use of X-ray structures of receptors and enzymes in drug discovery, and the contribution of molecular biology to drug discovery.
* Guidelines and operational strategems allowing identification of the portions of the molecule which are important for potency.
* The particular emphasis given to the three-dimensional aspects of the drug-receptor interactions, to the design of peptidomimetic drugs and to the control of the agonist-antagonist transition.
* Chemical solutions to solubility and to formulation problems. These sections cover perhaps the most neglected areas in medicinal chemistry books.
* Development of new drugs: legal and economic aspects constitutes another important area in which chemists are almost wholly self taught following their entry into industry.
Highly recommended to organic chemists entering into pharmaceutical research and to medicinal chemists in general.

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

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Published by Academic Press (1996)
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Published by Academic Press (1996)
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