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Discovery of GS-9256: A novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity

Authors :
Sheng, X. Christopher
Casarez, Anthony
Cai, Ruby
Clarke, Michael O.
Chen, Xiaowu
Cho, Aesop
Delaney, William E.
Doerffler, Edward
Ji, Mingzhe
Mertzman, Michael
Pakdaman, Rowchanak
Pyun, Hyung-Jung
Rowe, Tanisha
Wu, Qiaoyin
Xu, Jie
Kim, Choung U.
Source :
Bioorganic & Medicinal Chemistry Letters. Feb2012, Vol. 22 Issue 3, p1394-1396. 3p.
Publication Year :
2012

Abstract

Abstract: A potent and novel class of phosphinic acid derived product-like inhibitors of the HCV NS3/4A protease was discovered previously. Modification of the phosphinic acid and quinoline heterocycle led to GS-9256 with potent cell-based activity and favorable pharmacokinetic parameters. Based on these attributes, GS-9256 was advanced to human clinical trial as a treatment for chronic infection with genotype 1 HCV. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
22
Issue :
3
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
71334780
Full Text :
https://doi.org/10.1016/j.bmcl.2011.12.038