Novel,potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures |
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| Authors: | Orvieto Federica Koch Uwe Matassa Victor G Muraglia Ester |
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| Institution: | Medicinal Chemistry Department, IRBM-MRL Rome, V Pontina Km 30,600, 00040 Pomezia, Rome, Italy. |
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| Abstract: | Synthesis of hybrid HCV NS3 protease/NS4A inhibitors having the 4,4-difluoroaminobutyric acid (difluoroAbu) phenethylamides as P1-P1' and quinolyloxyprolines as P2 fragments led to 7 (IC(50) 54 nM). Molecular modelling suggests that this potent tripeptide inhibitor utilizes interactions in the S1', S1, S2, S3 and S4 sites of the protease. |
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