Alpha-ketoamides, alpha-ketoesters and alpha-diketones as HCV NS3 protease inhibitors |
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| Authors: | Han W Hu Z Jiang X Decicco C P |
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| Institution: | Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Wilmington, DE 19880, USA. wei.han@dupontpharma.com |
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| Abstract: | Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. Alpha-ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 of 340 nM. |
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