title: Synthesis and In Vitro Activity of Polyhalogenated 2-phenylbenzimidazoles as a New Class of anti-MRSA and Anti-VRE Agents.
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 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.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Hakan
authors.initials: H
authors.lastname: Göker
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Cigdem
authors.initials: C
authors.lastname: Karaaslan
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Erciyes University, 38039 Kayseri, Turkey.
authors.forename: Mustafa Orhan
authors.initials: MO
authors.lastname: Püsküllü
authors.affiliation: Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Sulhiye
authors.initials: S
authors.lastname: Yildiz
authors.affiliation: Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Yalcin
authors.initials: Y
authors.lastname: Duydu
authors.affiliation: Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Aylin
authors.initials: A
authors.lastname: Üstündağ
authors.affiliation: Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Ankara University, Dogol Str, 06100 Ankara, Turkey.
authors.forename: Can Özgür
authors.initials: CÖ
authors.lastname: Yalcin
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D006219:Halogens / Q000737:chemistry*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D021241:Spectrometry, Mass, Electrospray Ionization; D020713:Vancomycin Resistance / Q000187:drug effects*
chemical_list: D001562:Benzimidazoles; D006219:Halogens; C117755:2-phenylbenzimidazole
keywords: 2-phenylbenzimidazoles; antistaphylococcal activity; methicillin-resistant Staphylococcus aureus; polyhalogenated benzimidazoles; vancomycin-resistant Enterococcus faecium