Hu Guo-qiang, Xie Song-qiang, Xu Qiu-ju, Huang Wen-long, Zhang Hui-bin, Huang Sheng-tang
College of Pharmacy of Henan University, Kaifeng 475004, China.
Yao Xue Xue Bao. 2005 Apr;40(4):337-9.
To study on synthesis and antibacterial activity evaluation of polyheterocycles.
The 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.
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.
Oxadiazoles incorporting pyridyl triazole ring may be a pharmacophor structure in the molecule for developing antibacterial candidate drugs.
研究多杂环化合物的合成及抗菌活性评价。
4-氨基-3-吡啶-3-基-4H-[1,2,4]三唑-5-硫醇与2-氯甲基-5-取代苯基-[1,3,4]恶二唑缩合得到相应的标题杂环胺，并采用杯碟扩散法初步评价其体外抗菌活性。
合成了12个新化合物，其结构经红外光谱、核磁共振氢谱、质谱和元素分析确证。生物活性筛选结果表明，所制备的大多数化合物具有良好的抗菌活性。
含吡啶基三唑环的恶二唑可能是分子中开发抗菌候选药物的药效团结构。
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