新型甲硝唑-苯腙类化合物的设计、合成及抗菌活性研究

Synthesis and Biological Evaluation of Novel Metronidazole-Hydrazone Derivatives as Potential Antibacterial Agents

以甲硝唑、对羟基苯甲醛及取代肼为原料,经过3步反应,以较高产率合成得到一类新型的甲硝唑-苯腙类化合物,其结构经~1HNMR、^(13)CNMR和元素分析确证,所得化合物经抗菌活性筛选研究。结果表明,大部分化合物都具有较强的抗菌活性。其中以(E)-4-(2-(4-(2-(2-甲基-5-硝基-1H-咪唑-1-基)乙氧基)苯亚甲基)肼基)苯磺酰胺活性最好,对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和枯草芽孢杆菌的最低抑制浓度分别为1.56、0.78、0.39和0.39μg/m L。

A series of novel metronidazole hydrazone derivatives were synthesized in high yields via three steps,by using metronidazole,4-hydroxybenzaldehy and corresponding appropriate hydrazines as raw material. The structures of the synthesized compounds were confirmed by1 HNMR,13CNMR and elemental analysis. The antibacterial activities of all synthesized compounds were evaluated. The results showed that most of the tested compounds showed potent antibacterial activities. Among these compounds,compound 3j exhibited most potent antibacterial activities against Escherichia coli,Pseudomonas aeruginosa,Staphylococcus aureus and Bacillus subtilis with minimum inhibitory concentration（ MIC） of 1. 56,0. 78,0. 39 and 0. 39 μg / mL,respectively.