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Informationen zum Autor Professor Dennis Smith has worked in the pharmaceutical industry for 32 years after gaining his Ph.D from the University of Manchester. For 20 years he was at Pfizer Global Research and Development, Sandwich where he was Vice President-Pharmacokinetics, Dynamics and Metabolism. For the past 2 years he has been a Pfizer Academic Research Fellow working on a part-time basis. His research interests and publications span all aspects of Drug Discovery and Development particularly where drug metabolism knowledge can impact on the design of more efficacious and safer drugs. During this 30-year span he has helped in the Discovery and Development of eight marketed NCEs. He has authored over 100 publications including two books. Klappentext This outstanding book provides insight into the metabolism, pharmacokinetics and toxicity (ADMET) of chemicals by dividing the subject into functional groups. Following a description of chemical space and general ADMET in a unique way, by referring to actual chemical structures (functional groups) which even influence the molecules, they are incorporated into, in a specific manner. Many of the groupings are characterise the pharmacology of the drugs and are essential for particular activity; they are also a major influence in changing ADMET characteristics. These changes follow a pattern, thus allowing medicinal chemists to understand likely changes and how these can be overcome. Each chapter describes drugs containing the group, why the group is there and the physiochemical properties of a functional group before detailing the ADMET issues. In addition prodrugs and biosioteres are described where possible which may give alternative ADMET outcomes. The final chapter looks at future needs in terms of chemistry and ADMET understanding. Written by a team of scientists from Pfizer the book will appeal to postgraduate medicinal chemists and those working in industry. Zusammenfassung Written by medicinal chemists and ADMET scientists with a combined experience of over 300 years this aid to discovering drugs provides detailed coverage on absorption! distribution! metabolism! excretion and toxicology issues associated with new drugs. Inhaltsverzeichnis Drug targets and their structural motifs; ADMET for the medicinal chemist; Carboxlic acids and their isosteres; Primary, secondary and tertiary amines and isosteres; Sulphonamide as an essential group; 1, 2 and 3 ring phenyl and heterocyclic cores; Heterocycles and phenyls as essential pharmacophore groups; Peptides and peptidomimetic cores; Peptides and peptidomimetics as functional groups; Transition state functions; Alcohols and carbonyls; Future targets and chemistry needs;...
