2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2010 Dec 15;20(24):7317-22. doi: 10.1016/j.bmcl.2010.10.071.
Charles Z Ding 1,  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 Kazmierski,  Matthew D Tallant,  Lois L Wright,  Gary K Smith,  Renae M Crosby,  Amy A Wang,  Zhi-Jie Ni,  Wuxin Zou,  Jon Wright
Affiliations

Affiliation

  • 1 Anacor Pharmaceuticals, Inc., Palo Alto, CA 94303, USA. charles.ding@gmail.com
PMID: 21067923 DOI: 10.1016/j.bmcl.2010.10.071
Abstract

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.

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