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

作者: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
来源:Bioorganic & Medicinal Chemistry Letters, 2012, 22(3): 1394-1396.
DOI:10.1016/j.bmcl.2011.12.038

摘要

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.

  • 出版日期2012-2-1