Synthesis and Antimicrobial Activity of 2-(4-((4-substituted phenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-arylacetamides

Kaushik CP; Krishan Kumar

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Synthesis and Antimicrobial Activity of 2-(4-((4-substituted phenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-arylacetamides

机译：2-（4-（（4-取代的苯氧基）甲基）-1H-1,2,3-三唑-1-基）-N-芳基乙酰胺的合成及抑菌活性

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2-(4-((4-substituted phenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-arylacetamides (7a-7j) were synthesized through copper(I)-catalyzed click reaction of 1-methyl-4-(prop-2-ynyloxy)benzene (3a) and 1-nitro-4-(prop-2-ynyloxy)benzene (3b) with 2-azido-N-arylacetamides. The structural confirmation of the synthesized compounds was carried out by using various spectral techniques (FT-IR, 1H-NMR, 13C-NMR, HRMS). The synthesized compounds which reflects in general the various 1,4-disubstituted 1,2,3-triazoles were screened for in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa (Gram negative bacteria), Bacillus subtilis, Staphylococcus aureus (Gram positive bacteria) and antifungal activity against Candida albicans, Aspergillus niger. Compound 7i displayed good antimicrobial activity against tested bacterial and fungal strains.

机译：通过铜（I）催化的点击反应合成了2-（4-（（4-取代的苯氧基）甲基）-1H-1,2,3-三唑-1-基）-N-芳基乙酰胺（7a-7j）。 1-甲基-4-（丙-2-炔氧基）苯（3a）和1-硝基-4-（丙-2-炔氧基）苯（3-b）与2-叠氮基-N-芳基乙酰胺。通过使用各种光谱技术（FT-IR，1H-NMR，13C-NMR，HRMS）进行合成化合物的结构确认。筛选出一般反映各种1,4-二取代的1,2,3-三唑的合成化合物，它们对大肠杆菌，铜绿假单胞菌（革兰氏阴性菌），枯草芽孢杆菌，金黄色葡萄球菌（革兰氏阳性菌）具有体外抗菌活性。对白色念珠菌，黑曲霉的抗真菌活性。化合物7i对测试的细菌和真菌菌株显示出良好的抗菌活性。

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《Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry》 |2017年第11期|共6页
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Kaushik CP; Krishan Kumar;
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Synthesis and Antimicrobial Activity of 2-(4-((4-substituted phenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-arylacetamides

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