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依据生物活性叠加原理,将邻羟苯基、吡唑啉酮、苯腙基团进行合理组合,构建并合成了2-取代苯腙基-3-(2-羟基苯甲酰腙基)-丁酸乙酯(3a～3f)和1-(2-羟基苯甲酰基)-3-甲基-4-取代苯腙基-吡唑啉酮(4a～4f)两类、共计12种化合物,其中8种化合物未见报道,12种化合物的抑菌活性均未见报道.以芳胺为原料,经重氮化、与乙酰乙酸乙酯反应,与水杨酰肼缩合制得3a～3f,3a～3f经分子内关环制得4a～4f,化合物的结构经IR,1HNMR,元素分析等证实.生物活性测试表明,质量浓度为0.01%时,化合物3b,3c对大肠杆菌的抑菌率高达100%,具有很强的抑菌活性;化合物3a～3f对白色念珠菌、金黄色葡萄球菌的抑菌率均达70%以上,具有较强的抑菌活性;化合物4a～4f对白色念珠菌、大肠杆菌的抑菌率均接近或达到100%,具有很强的抑菌活性,对金黄色葡萄球菌的抑菌率均达78%以上,具有较强抑菌活性;与3a～3f相比,形成吡唑啉酮环后的化合物4a～4f的抗菌活性更高.
According to the principle of superposition of biological activity, o-hydroxyphenyl, pyrazolone and phenylhydrazone groups were combined rationally to construct and synthesize 2-substituted phenylhydrazone-3- (2-hydroxybenzoyl hydrazone) There are 12 compounds in total, which are ethyl acetate (3a ~ 3f) and 1- (2-hydroxybenzoyl) -3-methyl-4-substituted phenylhydrazono-pyrazolones (4a ~ 4f) Eight compounds have not been reported, and the antibacterial activities of the 12 compounds have not been reported.An arylamine was used as the raw material, diazotized, reacted with ethyl acetoacetate and condensed with salicylic hydrazide to prepare 3a ~ 3f, 3a ~ 3f The structures of 4a ~ 4f were confirmed by IR, 1HNMR and elemental analysis.The bioassay showed that the antibacterial activity of compounds 3b and 3c to Escherichia coli was as high as 100% when the mass concentration was 0.01% , And had strong antibacterial activity. The inhibitory rates of compounds 3a-3f against Candida albicans and Staphylococcus aureus were more than 70%, and had a strong antibacterial activity. Compounds 4a-4f showed inhibitory activity against Candida albicans, Bacteriostasis rate is close to or reach 100%, has a strong antibacterial activity, the antibacterial rate of Staphylococcus aureus were up to 78%, with strong antibacterial activity; compared with 3a ~ 3f, The compounds 4a-4f formed after the pyrazolone ring showed higher antibacterial activity.