胡国强, 谢松强, 许秋菊, 黄文龙, 张惠斌, 黄胜堂. 3-(5-取代苯基-[1,3,4]恶二唑-2-亚甲硫基)-5-吡啶-3-基-[1,2,4]三唑-4-胺的合成及抗菌活性J. 药学学报, 2005, 40(4): 337-339.
引用本文: 胡国强, 谢松强, 许秋菊, 黄文龙, 张惠斌, 黄胜堂. 3-(5-取代苯基-[1,3,4]恶二唑-2-亚甲硫基)-5-吡啶-3-基-[1,2,4]三唑-4-胺的合成及抗菌活性J. 药学学报, 2005, 40(4): 337-339.
HU Guo-qiang, XIE Song-qiang, XU Qiu-ju, HUANG Wen-long, ZHANG Hui-bin, HUANG Sheng-tang. Synthesis and antibacterial activity of 3-(5-substituted phenyl-[1,3,4]oxadiazole-2-yl-methylenethio)-5-pyridin-3-yl-[1,2,4] triazole-4-yl-aminesJ. Acta Pharmaceutica Sinica, 2005, 40(4): 337-339.
Citation: HU Guo-qiang, XIE Song-qiang, XU Qiu-ju, HUANG Wen-long, ZHANG Hui-bin, HUANG Sheng-tang. Synthesis and antibacterial activity of 3-(5-substituted phenyl-[1,3,4]oxadiazole-2-yl-methylenethio)-5-pyridin-3-yl-[1,2,4] triazole-4-yl-aminesJ. Acta Pharmaceutica Sinica, 2005, 40(4): 337-339.

3-(5-取代苯基-[1,3,4]恶二唑-2-亚甲硫基)-5-吡啶-3-基-[1,2,4]三唑-4-胺的合成及抗菌活性

Synthesis and antibacterial activity of 3-(5-substituted phenyl-[1,3,4]oxadiazole-2-yl-methylenethio)-5-pyridin-3-yl-[1,2,4] triazole-4-yl-amines

  • 摘要: 目的研究多杂环化合物的合成方法和抗菌活性。方法用4-氨基-3-吡啶-3-基-[1,2,4]三唑-5-硫醇与5-取代苯基-2-氯甲基-[1,3,4]恶二唑缩合得相应的目标胺类化合物。用平皿试验法,研究了目标化合物的体外抑菌活性。结果合成了12个新化合物,其结构经MS,IR,1H NMR和元素分析确证。多数化合物在体外表现出较好的抑菌活性。结论含吡啶的恶二唑三唑多杂环化胺类化合物有可能成为新型结构的抗菌药物。

     

    Abstract: AimTo study on synthesis and antibacterial activity evaluation of polyheterocycles. MethodsThe condensation of 4-amino-3-pyridin-3-yl-4H-[1,2,4] triazole-5-thiol with 2-chloromethyl-5-substituted phenyl-[1,3,4]oxadiazoles gave the corresponding title heterocycle amines, and the in vitro antibacterial activity was primarily evaluated by the method of cup-plate diffusion solution. Results Twelve novel compounds were synthesized, and their structures were confirmed by IR, 1H NMR, MS and element analysis. Biological screening results demonstrated that most of the compounds prepared showed good antibacterial activity. ConclusionOxadiazoles incorporting pyridyl triazole ring may be a pharmacophor structure in the molecule for developing antibacterial candidate drugs.

     

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