Synthesis and potent in vitro activity of novel 1H-benzimidazoles as anti-MRSA agents

Chem Biol Drug Des. 2012 Aug;80(2):237-44. doi: 10.1111/j.1747-0285.2012.01393.x. Epub 2012 Apr 30.

Abstract

A new class of 1H-benzimidazolecarboxamidines was synthesized and evaluated for in vitro antibacterial and antifungal activities, including drug-resistant bacterial strains. The most potent compound (32) has the same ratio of anti-MRSA activity as Vancomycin (minimal inhibitory concentrations value 0.78 μg/mL). The mechanism of action for 1H-benzimidazolecarboxamidine appears to be different from existing antibacterial agents. These compounds have potential for development as a new class of potent anti-MRSA agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology*
  • Candida / drug effects
  • Candidiasis / drug therapy
  • Humans
  • Methicillin Resistance / drug effects
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Staphylococcal Infections / drug therapy
  • Vancomycin / pharmacology

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Benzimidazoles
  • Vancomycin