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Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
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.
Affiliation
  • Sheng XC; Gilead Sciences, Inc., 333 Lakeside Dr, Foster City, CA 94404, USA. csheng@gilead.com
Bioorg Med Chem Lett ; 22(7): 2629-34, 2012 Apr 01.
Article in En | MEDLINE | ID: mdl-22366653
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Quinolines / Carboxylic Acids / Serine Proteinase Inhibitors / Viral Nonstructural Proteins / Hepacivirus Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Year: 2012 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Quinolines / Carboxylic Acids / Serine Proteinase Inhibitors / Viral Nonstructural Proteins / Hepacivirus Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Year: 2012 Document type: Article