2. Academic Validation
  3. Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease

Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease

  • Bioorg Med Chem Lett. 2012 Apr 1;22(7):2629-34. doi: 10.1016/j.bmcl.2012.01.017.
X Christopher Sheng 1,  Todd Appleby,  Thomas Butler,  Ruby Cai,  Xiaowu Chen,  Aesop Cho,  Michael O Clarke,  Jeromy Cottell,  William E Delaney 4th,  Edward Doerffler,  John Link,  Mingzhe Ji,  Rowchanak Pakdaman,  Hyung-Jung Pyun,  Qiaoyin Wu,  Jie Xu,  Choung U Kim
Affiliations

Affiliation

  • 1 Gilead Sciences, Inc., 333 Lakeside Dr, Foster City, CA 94404, USA. csheng@gilead.com
PMID: 22366653 DOI: 10.1016/j.bmcl.2012.01.017
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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