Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
复制标题
DOI：
10.1016/j.bmcl.2010.10.071
复制
发表时间：
2010-12-15
影响因子：
2.7
通讯作者：
Wright, Jon
中科院分区：
文献类型：
--
作者：
Ding, Charles Z.;Zhang, Yong-Kang;Wright, Jon
我们在此公开了一系列β 4-苯并氧杂硼杂环戊烯取代的大环HCV蛋白酶抑制剂。这些抑制剂对HCV NS 3蛋白酶是有效的，它们的抗HCV复制子效力在很大程度上受苯并氧杂硼杂环戊烯环系统和P2* 基团上的取代的影响。P2* 2-噻唑-异喹啉提供最佳复制子效力。本文描述了所选化合物的体外SAR研究和体内PK评价。(C)2010爱思唯尔有限公司版权所有。
We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2* groups. P2* 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein. (C) 2010 Elsevier Ltd. All rights reserved.