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本文以3-乙酰吲哚、草酸二乙酯、水合肼等为原料,经缩合、环化、水解反应制备3-(吲哚-3-基)吡唑-5-甲酸,后者再与苄胺或2-苯乙胺在EDC-BTOH催化下合成了一系列N-取代苄基-3-(吲哚-3-基)吡唑-5-甲酰胺和N-(2-取代苯基乙基)-3-(吲哚-3-基)吡唑-5-甲酰胺。采用平板计数法测试了化合物对大肠杆菌和金黄色葡萄球菌的抑制活性,结果表明,在浓度为80μg/m L时部分化合物有较高的抑菌活性。
In this paper, 3- (indol-3-yl) pyrazole-5-carboxylic acid was prepared by condensation, cyclization and hydrolysis from 3-acetylindole, diethyl oxalate and hydrazine hydrate. A series of N-substituted benzyl-3- (indol-3-yl) pyrazole-5-carboxamides and N- (2-substituted phenylethanolamines) were synthesized under the catalysis of EDC- Yl) -3- (indol-3-yl) pyrazole-5-carboxamide. The inhibitory activity of the compounds against Escherichia coli and Staphylococcus aureus was tested by plate counting method. The results showed that some of the compounds showed high antibacterial activity at the concentration of 80μg / mL.