Synthesis and evaluation of novel potent HCV NS5A inhibitors.

Synthesis and evaluation of novel potent HCV NS5A inhibitors.
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新型强效 HCV NS5A 抑制剂的合成和评价。

DOI:
10.1016/j.bmcl.2012.05.039
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发表时间:
2012
影响因子:
2.7
通讯作者:
Schinazi,RaymondF
Schinazi,RaymondF
中科院分区:
医学4区
文献类型:
--
作者:
Zhang,Hongwang;Zhou,Longhu;Amblard,Franck;Shi,Junxing;Bobeck,DrewR;Tao,Sijia;McBrayer,TamaraR;Tharnish,PhillipM;Whitaker,Tony;Coats,StevenJ;Schinazi,RaymondF

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Judicious modifications to the structure of the previously reported HCV NS5A inhibitor 1, resulted in more potent anti-HCV compounds with similar and in some cases improved toxicity profiles. The synthesis of 19 new NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. For the most potent compounds chemical stability, stability in liver microsomes and inhibition of relevant CYP450 enzymes is also presented.
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