Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373426 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
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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Related Topics
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Authors
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,