本文以对称二氨基硫脲为原料,经关环,缩合,亲核取代反应,合成出5个新型抗菌剂-3-取代硫基-4-N -邻羟苯基亚胺基-5-乙基-1,2,4-三唑类化合物(3a ～3e),并利用1HNMR,IR等进行结构表征.生物活性测试表明,质量浓度为0.01％时,3a ～3e对金黄色葡萄球菌与白色念珠茵的抑菌率均高于90.0％；对大肠杆菌的抑茵率高于80％.构效关系表明,三唑硫醚类化合物对革兰氏阳性茵(金黄色葡萄球菌)的抑制效果强于三唑硫醇类化合物；苯乙酰胺环的对位上引入拉电子基团如- Cl,- Br,- NO2可增加化合物的抑菌活性,而引入推电子基团如- CH3则降低其抑茵活性；与现售药物氟康唑相比,所合成的目标化合物的抗茵效果更优.%Five novel antibacterial agent - 3 - substituted sulfur-4-N - (2 - hydroxyphenyl) imino-5-ethyl-l ,2,4-triazole (3a~3e) were designed and synthesized by cyclization, condensation and nucleophilic substitution reaction. The structures of all compounds were characterized by IR and 'H NMR. The results of preliminary bioassay showed that, Compounds 3a ~3e have more than 90% inhibitory rate against Staphylococcus aureus and Monilia albican at 0. 01% mass concentration, which displayed excellent bacterial activities. The title Compounds have more than 80% inhibitory rate against Escherichia coli. QSAR analysis showed that the inhibitory of sulfide compounds against gram - positive bacteria ( Staphylococcus aureus ) is stronger than that of thiol compounds; The introduction of - Cl, - Br, - NO2 groups can effectively increase the antibacterial activity of compounds, and the introduction of - CH3 groups reduce its antibacterial activity; The antibacterial activity of target compounds is better than fluconazole.
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