Glycine alpha-ketoamides as HCV NS3 protease inhibitors |
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| Authors: | Han Wei Hu Zilun Jiang Xiangjun Wasserman Zelda R Decicco Carl P |
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| Institution: | Department of Discovery Chemistry, Pharmaceutical Research Institute, Bristol-Myers Squibb Company, PO Box 5400, Princeton, NJ 08543, USA. wei.han1@bms.com |
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| 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. |
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