Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease |
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| Authors: | Chen Kevin X Njoroge F George Prongay Andrew Pichardo John Madison Vincent Girijavallabhan Viyyoor |
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| Institution: | Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-3-3545, Kenilworth, NJ 07033, USA. kevin.chen@spcorp.com |
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| Abstract: | The 17-membered phenylalanine-based macrocycle 6 was prepared starting from 3-iodo-phenylalanine. Macrocyclization of alkene phenyl iodide 5 was effected through a palladium-catalyzed Heck reaction. The macrocyclic alpha-ketoamides were active inhibitors of the HCV NS3 protease, with the C-terminal acids and amides being more potent than tert-butyl esters. |
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