第二代丙型肝炎病毒NS3/4A丝氨酸蛋白酶抑制剂研究进展

Progress on the second generation inhibitors of hepatitis C virus NS3/4A serine protease

本文综述了近年来基于特拉匹韦(telaprevir)、波西匹韦(boceprevir)和BILN-2061等第一代HCV NS3/4A丝氨酸蛋白酶抑制剂的第二代抑制剂的结构改造。第二代抑制剂可有效提高抑制效力,显著改善药代动力学参数,可在一定程度上克服由第一代抑制剂诱导产生的耐药性。同时探讨了各类抑制剂的构效关系。

The progress of the second generation inhibitors of HCV NS3/4A serine protease, based on the modifications to the first generation ones （telaprevir, boceprevir, BILN-2061）,is reviewed. The second generation inhibitors can significantly improve potency,pharmacokinetic profiles, and to some degree reduce the resistance induced by the first generation ones. The structure-activi relationships of these inhibitors are also discussed.