2. Academic Validation
  3. Synthesis and evaluation of novel potent HCV NS5A inhibitors

Synthesis and evaluation of novel potent HCV NS5A inhibitors

  • Bioorg Med Chem Lett. 2012 Jul 15;22(14):4864-8. doi: 10.1016/j.bmcl.2012.05.039.
Hongwang Zhang 1,  Longhu Zhou,  Franck Amblard,  Junxing Shi,  Drew R Bobeck,  Sijia Tao,  Tamara R McBrayer,  Phillip M Tharnish,  Tony Whitaker,  Steven J Coats,  Raymond F Schinazi
Affiliations

Affiliation

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Decatur, GA 30033, USA.
PMID: 22704887 DOI: 10.1016/j.bmcl.2012.05.039
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.

Figures