Synthesis and anti-hepatitis B virus activity of a novel class of thiazolylbenzimidazole derivatives

Arch Pharm (Weinheim). 2011 Feb;344(2):78-83. doi: 10.1002/ardp.201000167. Epub 2010 Dec 22.

Abstract

Recently, heterocyclic benzimidazole derivatives have been investigated and validated as a promising class of antiviral agents. In this paper, a series of novel thiazolylbenzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity on the HepG2.2.15 cell line. Afterwards, the preliminary structure-activity relationship (SAR) was discussed. Compound 8b, with IC(50) = 1.1 µM and SI > 90.9, was the most promising compound and could be selected as a benchmark compound for further investigation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Antiviral Agents / toxicity
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Benzimidazoles / toxicity
  • Cell Death / drug effects
  • Drug Screening Assays, Antitumor / methods
  • Hep G2 Cells / drug effects
  • Hepatitis B virus / drug effects*
  • Humans
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests / methods
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Benzimidazoles