Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease
- 作者：X. Christopher Sheng ; csheng@gilead.com ; Todd Appleby ; Thomas Butler ; Ruby Cai ; Xiaowu Chen ; Aesop Cho ; Michael O. Clarke ; Jeromy Cottell ; William E. Delaney IV ; Edward Doerffler ; John Link ; Mingzhe Ji ; Rowchanak Pakdaman ; Hyung-Jung Pyun ; Qiaoyin Wu ; Jie Xu ; Choung U. Kim
- 关键词：HCV ; GS-9451 ; NS3 Protease ; Solubilizing group
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 April, 2012
- 卷：22
- 期：7
- 页码：2629-2634
- 文件大小：1032 K
摘要
The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV NS3 protease inhibitors with greatly improved pharmacokinetic properties in rats, dogs and monkeys.