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Glycine alpha-ketoamides as HCV NS3 protease inhibitors
Wei Han1, Zilun Hu, Xiangjun Jiang
1Department of Discovery Chemistry, Pharmaceutical Research Institute, Bristol-Myers Squibb Company, PO Box 5400, Princeton, NJ 08543, USA. wei.han1@bms.com
Bioorganic & Medicinal Chemistry Letters
|March 20, 2003
Abstract:
Using a tetrapeptide-based alpha-ketoamide template, various amines and amino acids were incorporated to explore the prime side of the HCV NS3 protease catalytic site. Glycine carboxylic acid was found to be the most effective prime group. Further optimization yielded an inhibitor with IC(50) of 0.060 microM.