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Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease |
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| Authors: | Li Xianfeng Zhang Yong-Kang Liu Yang Zhang Suoming Ding Charles Z Zhou Yasheen Plattner Jacob J Baker Stephen J Liu Liang Bu Wei Kazmierski Wieslaw M Wright Lois L Smith Gary K Jarvest Richard L Duan Maosheng Ji Jing-Jing Cooper Joel P Tallant Matthew D Crosby Renae M Creech Katrina Ni Zhi-Jie Zou Wuxin Wright Jon |
| Institution: | Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA. xli@anacor.com |
| 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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