State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
Eur J Med Chem. 2013 Jul;65:456-63. doi: 10.1016/j.ejmech.2013.05.004. Epub 2013 May 15.
A series of novel 1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives had been designed, synthesized, isolated and evaluated as potentiators of antibacterial agents. All these synthesized compounds were determined by elemental analysis, (1)H NMR, and MS. Their biological activities were also evaluated against two Gram-negative bacterial strains: Escherichia coli and Pseudomonas aeruginosa and two Gram-positive bacterial strains: Bacillus thuringiensis and Bacillus subtilis by MTT method as potential FabH inhibitory. The results showed that compound 30 exhibited the most potent E. coli FabH inhibitory activity with IC50 of 4.6 μM. Molecular modeling simulation studies were performed in order to predict the biological activities of the proposed compounds. All compounds have been tested for toxicity by MTT assay on human macrophage.
设计、合成、分离并评价了一系列新型 1-(2-羟丙基)-2-苯乙烯基-5-硝基咪唑衍生物，作为抗菌药物的增效剂。所有合成的化合物均通过元素分析、(1)H NMR 和 MS 进行了确定。通过 MTT 法测定了它们对两种革兰氏阴性菌（大肠杆菌和铜绿假单胞菌）和两种革兰氏阳性菌（苏云金芽孢杆菌和枯草芽孢杆菌）的生物活性，作为潜在的 FabH 抑制剂。结果表明，化合物 30 对大肠杆菌 FabH 的抑制活性最强，IC50 为 4.6 μM。为了预测所提出化合物的生物活性，进行了分子模拟模拟研究。所有化合物均通过 MTT 法在人巨噬细胞上进行了毒性测试。
