Perspectives in Medicinal Chemistry ![](images/rss-icon.gif)
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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