title: Synthesis and potent in vitro activity of novel 1H-benzimidazoles as anti-MRSA agents.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.
authors.forename: Hacer
authors.initials: H
authors.lastname: Karataş
authors.forename: Mehmet
authors.initials: M
authors.lastname: Alp
authors.forename: Sulhiye
authors.initials: S
authors.lastname: Yildiz
authors.forename: Hakan
authors.initials: H
authors.lastname: Göker
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects; D002177:Candidiasis / Q000188:drug therapy; D006801:Humans; D016106:Methicillin Resistance / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D013203:Staphylococcal Infections / Q000188:drug therapy; D014640:Vancomycin / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001562:Benzimidazoles; D014640:Vancomycin