Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: non-symmetric inhibitors with potent activity against genotype 1a and 1b

Bioorg Med Chem Lett. 2015 Feb 15;25(4):940-3. doi: 10.1016/j.bmcl.2014.12.044. Epub 2014 Dec 29.

Abstract

The discovery of non-symmetric thienoimidazole-containing HCV NS5A inhibitors is described. The inhibitors herein reported display high potencies against both genotype 1a and 1b. In this follow-up manuscript, we discuss the importance of the linker aromaticity to achieve high potency, particularly against genotype 1a.

Keywords: HCV; Hepatitis C; NS5A; Thienoimidazole.

MeSH terms

  • Animals
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Genotype
  • Hepacivirus / drug effects*
  • Hepacivirus / genetics
  • Humans
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Rats
  • Viral Nonstructural Proteins / drug effects*

Substances

  • Antiviral Agents
  • Imidazoles
  • Viral Nonstructural Proteins
  • NS-5 protein, hepatitis C virus