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Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease |
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| Authors: | Sheng X Christopher Appleby Todd Butler Thomas Cai Ruby Chen Xiaowu Cho Aesop Clarke Michael O Cottell Jeromy Delaney William E Doerffler Edward Link John Ji Mingzhe Pakdaman Rowchanak Pyun Hyung-Jung Wu Qiaoyin Xu Jie Kim Choung U |
| Institution: | Gilead Sciences, Inc., 333 Lakeside Dr, Foster City, CA 94404, USA. csheng@gilead.com |
| Abstract: | 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. |
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