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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

2011; Elsevier BV; Volume: 22; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2011.12.038

1464-3405

X. Christopher Sheng, Anthony Casarez, Ruby Cai, Michael O. Clarke, Xiaowu Chen, Aesop Cho, William E. Delaney, Edward Doerffler, Mingzhe Ji, Michael Mertzman, Rowchanak Pakdaman, Hyung‐Jung Pyun, Tanisha Rowe, Qiaoyin Wu, Jie Xu, Choung U. Kim,

Hepatitis B Virus Studies

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.