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化学进展  2012 

非核苷类HCVNS5B聚合酶抑制剂

, PP. 2255-2267

Keywords: 丙型肝炎病毒(HCV),特异性靶向药物,NS5B聚合酶,非核苷类抑制剂

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Abstract:

全球约有1.7亿人感染丙型肝炎病毒(HCV),至今尚无有效的疫苗和治疗药物。目前干扰素-α和利巴韦林联用抗HCV的标准治疗方案存在严重不良反应。近年来,新型抗HCV的研究主要集中于针对病毒感染的特异性靶点寻找新的抑制剂。NS5B聚合酶因其在HCVRNA基因组复制中的关键性作用,是目前抗HCV药物设计的重要靶点之一。NS5B聚合酶抑制剂可分为核苷类抑制剂(NIs)和非核苷类抑制剂(NNIs)。自从第一个NS5BNNIs苯并咪唑类化合物被报道以来,大量不同结合位点NS5BNNIs相继被报道,一些化合物在临床研究中表现出了可喜的疗效。本文综述了苯并噻二嗪类、苯并咪唑类、吲哚类、噻吩羧酸类、喹啉酮类、二氢吡喃类和二酮酸类等NS5BNNIs的研究进展,旨在为该类抑制剂的开发研究提供参考。

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