Synthesis and Potent In vitro Activity of Novel 1H-Benzimidazoles as Anti-MRSA Agents

Karataş H., ALP M., YILDIZ S., GÖKER A. H.

Chemical Biology and Drug Design, vol.80, no.2, pp.237-244, 2012 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 80 Issue: 2
  • Publication Date: 2012
  • Doi Number: 10.1111/j.1747-0285.2012.01393.x
  • Journal Name: Chemical Biology and Drug Design
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.237-244
  • Keywords: 1H-Benzimidazole, antifungal and antibacterial activities, benzamide, benzamidine, methicillin-resistant Staphylococcus aureus, ANTIMICROBIAL ACTIVITY, STAPHYLOCOCCUS-AUREUS, ANTIBACTERIAL AGENTS, VRE AGENTS, BENZIMIDAZOLES
  • Lokman Hekim University Affiliated: No

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 0.78μg/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. © 2012 John Wiley & Sons A/S.