Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

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• 作者：Charles Z. Ding ; Yong-Kang Zhang ; Xianfeng Li ; Yang Liu ; Suoming Zhang ; Yasheen Zhou ; Jacob J. Plattner ; Stephen J. Baker ; Liang Liu ; Maosheng Duan ; Richard L. Jarvest ; Jingjing Ji ; Wieslaw M. Kazmier
• 关键词：HCV ; HCV protease inhibitors ; Benzoxaborole ; Synthesis and biological evaluations ; HCV NS3 protease inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 December 2010
• 年：2010
• 卷：20
• 期：24
• 页码：7317-7322
• 全文大小：662 K

文摘

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.