New 7-Piperazinylquinolones Containing (Benzo[D]Imidazol-2-Yl)Methyl Moiety As Potent Antibacterial Agents Publisher Pubmed



Arab HA¹ ; Faramarzi MA² ; Samadi N³ ; Irannejad H⁴ ; Foroumadi A⁵ ; Emami S⁴ Show Affiliations
Source: Molecular Diversity Published:2018

Abstract

A series of 7-piperazinylquinolones containing a (benzo[d]imidazol-2-yl)methyl moiety were designed and synthesized as new antibacterial agents. The antibacterial activity of title compounds was evaluated against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia) microorganisms. Among the tested compounds, the N1-cyclopropyl derivative 4a showed the highest activity against S. aureus, S. epidermidis, B. subtilis and E. coli (MIC = 0.097 μ g/mL), being 2–4 times more potent than reference drug norfloxacin. A structure-activity relationship study demonstrated that the effect of the nitro group on the benzimidazole ring depends on the pattern of substitutions on the piperazinylquinolone. © 2018, Springer International Publishing AG, part of Springer Nature.