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


Goker H., Karaaslan C., PÜSKÜLLÜ M. O., Yildiz S., Duydu Y., Ustundag A., ...More

CHEMICAL BIOLOGY & DRUG DESIGN, vol.87, no.1, pp.57-68, 2016 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 87 Issue: 1
  • Publication Date: 2016
  • Doi Number: 10.1111/cbdd.12623
  • Journal Name: CHEMICAL BIOLOGY & DRUG DESIGN
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • 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
  • Erciyes University Affiliated: Yes

Abstract

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 mu g/mL) with the lowest MIC values with 0.19 mu g/mL against methicillin-resistant Staphylococcus aureus, 8 and 35 exhibited best inhibitory activity against vancomycin-resistant Enterococcus faecium (1.56 mu g/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.