Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease
2012; Elsevier BV; Volume: 22; Issue: 7 Linguagem: Inglês
10.1016/j.bmcl.2012.01.017
ISSN1464-3405
AutoresX. Christopher Sheng, T.C. Appleby, Thomas Butler, Ruby Cai, Xiaowu Chen, Aesop Cho, Michael O. Clarke, Jeromy J. Cottell, William E. Delaney, Edward Doerffler, John O. Link, Mingzhe Ji, Rowchanak Pakdaman, Hyung‐Jung Pyun, Qiaoyin Wu, Jie Xu, Choung U. Kim,
Tópico(s)Hepatitis B Virus Studies
ResumoThe 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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