发现一种可逆转的 HCV NS5B 聚合酶抑制剂。
Discovery of an irreversible HCV NS5B polymerase inhibitor.
机构信息
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6.
PMID:24252545
Abstract
The discovery of lead compound 2e was described. Its covalent binding to HCV NS5B polymerase enzyme was investigated by X-ray analysis. The results of distribution, metabolism and pharmacokinetics were reported. Compound 2e was demonstrated to be potent (replicon GT-1b EC50 = 0.003 μM), highly selective, and safe in in vitro and in vivo assays.
摘要
本文描述了先导化合物 2e 的发现。通过 X 射线分析研究了其与 HCV NS5B 聚合酶的共价结合。报告了分布、代谢和药代动力学的结果。在体外和体内试验中，化合物 2e 表现出强效（复制子 GT-1b EC50 = 0.003 μM）、高度选择性和安全性。
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