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
  • 1. Gilead Sciences, Inc., 333 Lakeside Dr, Foster City, CA 94404, USA. [email protected]
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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