Efficient synthesis, antitubercular and antimicrobial evaluation of 1,4-disubstituted 1,2,3-triazoles with amide functionality

被引：17

作者：

Kaushik, C. P. ^{[1
]}

Pahwa, Ashima ^{[1
]}

Singh, Dharmendra ^{[2
]}

Kumar, Krishan ^{[1
]}

Luxmi, Raj ^{[1
]}

机构：

[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar, Haryana, India

[2] IPCA Lab Ltd, Ctr Res & Dev, Mumbai, Maharashtra, India

来源：

MONATSHEFTE FUR CHEMIE | 2019年 / 150卷 / 06期

关键词：

Click reaction; Heterocycles; 1,4-Disubstituted; 1,2,3-Triazoles; Alkynes; One-pot synthesis; Biological activity; LINKED COUMARINYL TRIAZOLES; CLICK CHEMISTRY; ANTIMALARIAL; CYCLOADDITION; DERIVATIVES;

D O I：

10.1007/s00706-019-2361-9

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 21 amide linked 1,4-disubstituted-1,2,3-triazoles were achieved via one-pot synthesis through Cu(I) catalyzed click reaction between terminal alkynes and 2-azido-N-substituted acetamides. Newly formed triazoles were characterized by various spectroscopic techniques (FT-IR, H-1 NMR, C-13 NMR spectroscopy, and HRMS) and investigated for in vitro antitubercular evaluation against bacteria, i.e., Mycobacterium tuberculosis and antimicrobial evaluation against Bacillus subtilis, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, and Aspergillus niger. Some of the synthesized triazole derivatives were found to exhibit moderate inhibitory activity against the tested antitubercular strain, whereas one compound displayed a significant inhibitory activity against most of the tested microbial strains.

引用

页码：1127 / 1136

页数：10

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