Synthesis and in vitro activity of dicationic bis-benzimidazoles as a new class of anti-MRSA and anti-VRE agents

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1292-5. doi: 10.1016/j.bmcl.2009.01.075. Epub 2009 Feb 7.

Abstract

A new class of novel bis-benzimidazole diamidine compounds have been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Anti-MRSA and anti-VRE activities of the most potent compound 1 were more active than Vancomycin. The mechanism of action for this class of compounds appears to be different from existing antibiotics. Bis-benzimidazole diamidine compounds have potential for further investigation as a new class of potent anti-MRSA and anti-VRE agents.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / classification
  • Anti-Bacterial Agents / pharmacology
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / classification
  • Benzimidazoles / pharmacology*
  • Drug Resistance, Multiple, Bacterial / drug effects
  • Enterococcus faecium / drug effects*
  • Methicillin Resistance / drug effects
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship
  • Vancomycin Resistance / drug effects

Substances

  • Anti-Bacterial Agents
  • Benzimidazoles
  • bis-benzimidazole