发现4H-吡唑并[1,5-a]嘧啶-7-酮作为丙型肝炎病毒聚合酶的有效抑制剂。
Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase.
作者信息
Deng Yongqi, Shipps Gerald W, Wang Tong, Popovici-Muller Janeta, Rosner Kristin E, Siddiqui M Arshad, Duca Jose, Cooper Alan B, Cable Michael
机构信息
Schering-Plough Research Institute Cambridge, 320 Bent Street, Cambridge, MA 02141, United States.
出版信息
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5363-7. doi: 10.1016/j.bmcl.2009.07.124. Epub 2009 Aug 6.
PMID:19682898
Abstract
A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase. A number of these compounds exhibited potent activity in enzymatic assay. The synthesis and structure-activity relationship are also described.
摘要
合成了一系列4H-吡唑并[1,5-a]嘧啶-7-酮衍生物，并对其抗丙型肝炎病毒NS5B RNA依赖性RNA聚合酶的抑制活性进行了评估。其中许多化合物在酶活性测定中表现出强效活性。还描述了其合成及构效关系。
Zotero 插件