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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Li X,Zhang YK,Liu Y,Zhang S,Ding CZ,Zhou Y,Plattner JJ,Baker SJ,Liu L,Bu W,Kazmierski WM,Wright LL,Smith GK,Jarvest RL,Duan M,Ji JJ,Cooper JP,Tallant MD,Crosby RM,Creech K,Ni ZJ,Zou W,Wright J

doi

10.1016/j.bmcl.2010.10.007

subject

Has Abstract

pub_date

2010-12-15 00:00:00

pages

7493-7

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01458-7

journal_volume

20

pub_type

杂志文章

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