一些1,4-二取代1,2,3-三唑的合成及其抗菌活性

Belkheira Mokhtaria, El Abed Douniazad El Abed Douniazad
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引用次数: 1

摘要

我们在没有金属催化剂的情况下,采用氢胺化/1,3-偶极环加成的顺序反应,从末端炔和芳基酰胺开始,实现了1,4-二取代1,2,3-三唑的高选择性合成。合成产物的结构通过常用的光谱方法(红外光谱、1h NMR和13c NMR)进行了表征。对得到的1,2,3-三唑进行了抗菌性能测试。其中大部分对铜绿假单胞菌、弗氏柠檬酸杆菌、大肠杆菌、金黄色葡萄球菌有显著的抑菌活性,对黄曲霉和赭曲霉有明显的杀真菌活性。
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Synthesis and Antimicrobial Activity of some 1,4-Disubstituted 1,2,3-Triazoles
We realized the highly selective synthesis of 1,4-disubstituted 1,2,3-triazoles starting from a terminal alkyne and arylazides, without the presence of metal catalyst, using the sequence hydroamination/1,3-dipolar cycloaddition reaction. The structure of synthesized products was determined by the usual spectroscopic methods (IR, 1 H NMR and 13 C NMR). The 1,2,3-triazoles obtained were tested for their antimicrobial properties. Most of them showed a significant antibacterial activity against Pseudomonas aeruginosa, Citrobacter freundii, Escherichia coli, Staphylococcus aureus, and a fungicidal activity against Aspergillus flavus and Aspergillus ochraceus.
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