根据拼接原理将活性基团腙引入中药活性成分丹皮酚中对其结构进行修饰,以丹皮酚为原料,与80％水合肼在乙醇中反应得到中间体丹皮酚腙(2),然后与芳香醛反应合成了10个芳甲叉基丹皮酚腙(3a-3j),其结构经IR、1 H NMR、13 C NMR和ESI-MS表征.采用二倍稀释法测定目标化合物对金黄色葡萄球菌和大肠杆菌的最低抑菌浓度(MIC),结果表明:大部分化合物金黄色葡萄球菌和大肠杆菌表现出较好的抑菌活性,特别是化合物3i对金黄色葡萄球菌的的MIC为2μg·mL-1,优于阳性对照药环丙沙星.%Paeonol was modified by active functional group hydrazone according to the combination principle. The intermediate hydrazone(2)was synthesized by condensation reaction of paeonol with 80％ hydrazine hydrate in 95％ ethanol. Ten novel paeonol hydrazine compounds(3a-3j)were prepared by the reaction of 2 and appropriate arylaldehydes. Their structures were characterized by IR,1 H NMR,13 C NMR,and ESI-MS. The minimal inhibitory concentrations(MIC)of target compounds against S. aureus and E. coli. were determined by two times dilution method. The results showed that most of the tested compounds displayed good antimicro-bial activities. In particular,compound 3i exhibited better inhibitory activities than ciprofloxacin against S. aureus.
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