Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Mol Divers. 2018 Nov;22(4):815-825. doi: 10.1007/s11030-018-9834-3. Epub 2018 Jun 7.
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 ([Formula: see text] [Formula: see text]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.
一系列含有（苯并[d]咪唑-2-基）甲基部分的 7-哌嗪基喹诺酮被设计和合成，作为新型抗菌剂。标题化合物的抗菌活性针对革兰氏阳性（金黄色葡萄球菌、表皮葡萄球菌和枯草芽孢杆菌）和革兰氏阴性（大肠杆菌、铜绿假单胞菌和肺炎克雷伯菌）微生物进行了评估。在测试的化合物中，N1-环丙基衍生物 4a 对金黄色葡萄球菌、表皮葡萄球菌、枯草芽孢杆菌和大肠杆菌表现出最高的活性（[Formula: see text] [Formula: see text]g/mL），比参考药物诺氟沙星强 2-4 倍。构效关系研究表明，苯并咪唑环上硝基的作用取决于哌嗪基喹诺酮上取代基的模式。
