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. Epub 2012 May 24.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Hepacivirus / drug effects*
  • Humans
  • Microsomes, Liver / drug effects
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antiviral Agents