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[目的]设计合成新型的抗菌药物甲基2-(-(-5-苯亚甲基-4-噻唑酮-2-亚基)氨基)噻唑-5-羧酸酯类衍生物,并评价其抗菌活性.[方法]以2-氨基噻唑-5-甲酸甲酯与氯乙酰氯合成酰胺后与硫氰酸铵环合得到噻唑酮,而后与不同取代苯甲醛缩合得到相应的目标产物(4a~4l),并进行抗菌实验.[结果]所有合成的化合物结构均经IR,1 H-NMR进行了确证,其中4a,4j,4k对金黄色葡萄球菌S.a4220有较强的抑菌作用.[结论]合成的部分化合物表现出良好的抑菌活性.
[Objective] The purpose was to design and synthesize a novel antimicrobial methyl 2 - (- (- 5 - benzylidene - 4 - thiazolone - 2 - ylidene) amino) thiazole - 5 - carboxylate derivatives and evaluate [Method] The amide of 2-aminothiazole-5-carboxylic acid was reacted with chloroacetyl chloride to form thiazolone by cyclization with ammonium thiocyanate, then the corresponding target product was obtained by condensation with different substituted benzaldehydes (4a ~ 4l), and antibacterial experiments were carried out. [Results] The structures of all the synthesized compounds were confirmed by IR and 1 H-NMR. Among them, 4a, 4j and 4k showed strong antibacterial activity against S.aureus Staphylococcus aureus. [Conclusion] Some of the compounds synthesized showed good antibacterial activity.