1237745-86-6Relevant articles and documents
Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups
Li, Xianfeng,Liu, Yang,Zhang, Yong-Kang,Plattner, Jacob J.,Baker, Stephen J.,Bu, Wei,Liu, Liang,Zhou, Yasheen,Ding, Charles Z.,Zhang, Suoming,Kazmierski, Wieslaw M.,Hamatake, Robert,Duan, Maosheng,Wright, Lois L.,Smith, Gary K.,Jarvest, Richard L.,Ji, Jing-Jing,Cooper, Joel P.,Tallant, Matthew D.,Crosby, Renae M.,Creech, Katrina,Wang, Amy
, p. 7351 - 7356 (2012)
We have synthesized and evaluated a series of novel HCV NS3 protease inhibitors with various P4 capping groups, which include urea, carbamate, methoxy-carboxamide, cyclic carbamate and amide, pyruvic amide, oxamate, oxalamide and cyanoguanidine. Most of these compounds are remarkably potent, exhibiting single-digit to sub-nanomolar activity in the enzyme assay and cell-based replicon assay. Selected compounds were also evaluated in the protease-inhibitor-resistant mutant transient replicon assay, and they were found to show quite different potency profiles against a panel of HCV protease-inhibitor-resistant mutants.
COMPOUNDS
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Page/Page column 36, (2010/08/08)
The present invention features compounds of Formula (I) and (Ia), pharmaceutical compositions and use in the treatment of viral disease:
