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甲基2-(-(-5-苯亚甲基-4-噻唑酮-2-亚基)氨基)噻唑-5-羧酸酯类衍生物的合成及其抗菌活性研究

Synthesis and antibacterial activities of methyl 2-(-(-5-benzylidene-4-oxothiazolidin-2-ylidene)amino)thiazole-5-carboxylate
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摘要 [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. OBJECTIVETo designe and synthesize a series of methyl 2-（-（-5-benzylidene-4-oxothiazolidin-2-ylidene）amino）thiazole-5-carboxylate in order to find neotype antibacterials.METHODS Methyl 5-（2-chloroacetamido）thiophene-2-carboxylate 2was obtained by methyl 5-aminothiophene-2-carboxylate reaction with 2-chloracetyl chloride,and then cyclization with ammonium thiocyanate yielded 3.Condensation of 3with the corresponding benzaldehyde yielded 4a-4l,and the antibacterial experiment was perfoemed.RESULTSThe structure of target compounds were determined by IR,1 H-NMR,and in which 4a,4j,4kfor the staphylococcus aureusS.a 4220 had strong bacteriostatic action.CONCLUSIONPart of the synthesized compounds shows good bacteriostatic activity.
作者 李亚茹 郭萌 郑昌吉 朴虎日
机构地区 延边大学药学院
出处 《延边大学医学学报》 CAS 2015年第1期18-21,共4页 Journal of Medical Science Yanbian University
关键词 噻唑 噻唑酮 苯甲醛 抗菌活性 合成 thiazole thiazolone benzaldehyde antibacterial activity synthesis
分类号 R914 [医药卫生—药物化学]
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延边大学医学学报
2015年 第1期

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