Synthesis and evaluation of novel potent HCV NS5A inhibitors
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- 作者：Hongwang Zhang ; Longhu Zhou ; Franck Amblard ; Junxing Shi ; Drew R. Bobeck ; Sijia Tao ; Tamara R. McBrayer ; Phillip M. Tharnish ; Tony Whitaker ; Steven J. Coats ; Raymond F. Schinazi
- 关键词：NS5A ; Antiviral ; HCV
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：15 July, 2012
- 年：2012
- 卷：22
- 期：14
- 页码：4864-4868
- 全文大小：1425 K
文摘
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.