Perspectives in Medicinal Chemistry 
Perspectives in Medicinal Chemistry will publish articles that combine aspects of commentaries and reviews, allowing medicinal chemists to discuss drug design without the necessity of revealing proprietary information.
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Lead Optimization in Discovery Drug Metabolism and Pharmacokinetics/Case study: The Hepatitis C Virus (HCV) Protease Inhibitor SCH 503034
K.-C. Cheng1, Walter A. Korfmacher1, Ronald E. White1 and F. George Njoroge2
1Department of Drug Metabolism and Pharmacokinetics. 2Chemistry Department Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033 U.S.A.
Abstract: Lead optimization using drug metabolism and pharmacokinetics (DMPK) parameters has become one of the primary focuses of research organizations involved in drug discovery in the last decade. Using a combination of rapid in vivo and in vitro DMPK screening procedures on a large array of compounds during the lead optimization process has resulted in development of compounds that have acceptable DMPK properties. In this review, we present a general screening paradigm that is currently being used as part of drug discovery at Schering-Plough and we describe a case study using the Hepatitis C Virus (HCV) protease inhibitor program as an example. By using the DMPK optimization tools, a potent HCV protease inhibitor, SCH 503034, was selected for development as a candidate drug.
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