Synthesis and in Vitro Activity of Polyhalogenated 2-phenylbenzimidazoles as a New Class of anti-MRSA and Anti-VRE Agents


GÖKER A. H. , Karaaslan C., PÜSKÜLLÜ M. O. , YILDIZ S. , DUYDU Y., ÜSTÜNDAĞ A., ...More

Chemical Biology and Drug Design, vol.87, no.1, pp.57-68, 2016 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 87 Issue: 1
  • Publication Date: 2016
  • Doi Number: 10.1111/cbdd.12623
  • Title of Journal : Chemical Biology and Drug Design
  • Page Numbers: pp.57-68
  • Keywords: 2-phenylbenzimidazoles, antistaphylococcal activity, methicillin-resistant Staphylococcus aureus, polyhalogenated benzimidazoles, vancomycin-resistant Enterococcus faecium, POTENT ANTISTAPHYLOCOCCAL ACTIVITY, DRUG, HALOGENATION, INHIBITORS, MARIBAVIR

Abstract

© 2015 John Wiley & Sons A/S.A series of novel polyhalogenated 2-phenylbenzimidazoles have been synthesized and evaluated for in vitro antistaphylococcal activity against drug-resistant bacterial strains (methicillin-resistant Staphylococcus aureus, and vancomycin-resistant Enterococcus faecium. Certain compounds inhibit bacterial growth perfectly. 11 was active than vancomycin (0.78 μg/mL) with the lowest MIC values with 0.19 μg/mL against methicillin-resistant Staphylococcus aureus, 8 and 35 exhibited best inhibitory activity against vancomycin-resistant Enterococcus faecium (1.56 μg/mL). The mechanism of action for this class of compounds appears to be different than clinically used antibiotics. These polyhalogenated benzimidazoles have potential for further investigation as a new class of potent anti-methicillin-resistant Staphylococcus aureus and anti-vancomycin-resistant Enterococcus faecium agents.