title: Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines.
abstract: A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines (23-33) have been synthesized and evaluated for their potential antistaphylococcal activity. Cytotoxic effects of the compounds were investigated by the neutral red uptake (NRU) cytotoxicity test. Most of the compounds exhibited good MICs values against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Compound 28 with N-cyclohexylcarboxamidine group at the 5-position was found to be the most potent agent, with the MIC value of 3.12 µg/mL.
authors.affiliation: Department of Pharmaceutical Chemistry .
authors.forename: M Orhan
authors.initials: MO
authors.lastname: Püsküllü
authors.forename: Sulhiye
authors.initials: S
authors.lastname: Yıldız
authors.forename: Yalçın
authors.initials: Y
authors.lastname: Duydu
authors.forename: Aylin
authors.initials: A
authors.lastname: Üstündağ
authors.forename: Hakan
authors.initials: H
authors.lastname: Göker
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000900:Anti-Bacterial Agents; D001562:Benzimidazoles
keywords: 1H-benzimidazole-5-carboxamidines; 1H-benzimidazole-5-carboxylic acid; 1H-benzimidazole-5-sulfonamide; MRSA; antistaphylococcal activity