Synthesis and evaluation of novel potent HCV NS5A inhibitors

Authors :: Zhang, Hongwang
Zhou, Longhu
Amblard, Franck
Shi, Junxing
Bobeck, Drew R.
Tao, Sijia
McBrayer, Tamara R.
Tharnish, Phillip M.
Whitaker, Tony
Coats, Steven J.
Schinazi, Raymond F.
Source :: Bioorganic & Medicinal Chemistry Letters. 7/15/2012, Vol. 22 Issue 14, p4864-4868. 5p.
Publication Year :: 2012
Abstract: Abstract: Judicious modifications to the structure of the previously reported HCV NS5A inhibitor 1, resulted in more potent anti-HCV compounds with similar and in some cases improved toxicity profiles. The synthesis of 19 new NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. For the most potent compounds chemical stability, stability in liver microsomes and inhibition of relevant CYP450 enzymes is also presented. [Copyright &y& Elsevier]