Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-symmetric inhibitors with diyne and biphenyl linkers

Bioorg Med Chem Lett. 2015 Feb 15;25(4):936-9. doi: 10.1016/j.bmcl.2014.12.046. Epub 2014 Dec 30.

Abstract

The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the aromatic character of the linker to achieve high genotype 1a potency.

Keywords: HCV; Hepatitis C; NS5a; Thienoimidazole.

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Drug Discovery*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

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