Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

Bioorg Med Chem. 2010 Jul 15;18(14):5048-55. doi: 10.1016/j.bmc.2010.05.076. Epub 2010 Jun 1.

Abstract

A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology*
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Hepatitis B / drug therapy*
  • Hepatitis B virus / drug effects*
  • Humans
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Benzimidazoles