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Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease

✍ Scribed by Xianfeng Li; Yong-Kang Zhang; Yang Liu; Suoming Zhang; Charles Z. Ding; Yasheen Zhou; Jacob J. Plattner; Stephen J. Baker; Liang Liu; Wei Bu; Wieslaw M. Kazmierski; Lois L. Wright; Gary K. Smith; Richard L. Jarvest; Maosheng Duan; Jing-Jing Ji; Joel P. Cooper; Matthew D. Tallant; Renae M. Crosby; Katrina Creech; Zhi-Jie Ni; Wuxin Zou; Jon Wright

Book ID: 104004978
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 668 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.007

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✦ Synopsis

HCV NS3/4A serine protease is essential for the replication of the HCV virus and has been a clinically validated target. A series of HCV NS3/4A protease inhibitors containing a novel acylsulfamoyl benzoxaborole moiety at the P1' region was synthesized and evaluated. The resulting P1-P3 and P2-P4 macrocyclic inhibitors exhibited sub-nanomolar potency in the enzymatic assay and low nanomolar activity in the cell-based replicon assay. The in vivo PK evaluations of selected compounds are also described.

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