439692-05-4Relevant academic research and scientific papers
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 (2013/02/21)
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.
MACROCYCLIC SERINE PROTEASE INHIBITORS USEFUL AGAINST VIRAL INFECTIONS, PARTICULARLY HCV
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Page/Page column 166, (2011/02/24)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (Ia) or (Ib), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
MACROCYCLIC SERINE PROTEASE INHIBITORS
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, (2010/11/03)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
