Synthesis and antimicrobial evaluation of ester-linked 1,4-disubstituted 1,2,3-triazoles with a furyl/thienyl moiety

被引:22
作者
Kaushik, C. P. [1 ]
Luxmi, Raj [1 ]
Singh, Dharmendra [2 ]
Kumar, Ashwani [3 ]
机构
[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India
[2] IPCA Lab Ltd, Ctr Res & Dev, Bombay, Maharashtra, India
[3] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India
关键词
Antibacterial activity; Antifungal activity; Click chemistry; Disubstituted 1,2,3-triazoles; Synthesis; BIOLOGICAL EVALUATION; CLICK CHEMISTRY; ORGANIC AZIDES; 1,2,3-BISTRIAZOLES; INHIBITORS; DESIGN; AGENTS; DERIVATIVES;
D O I
10.1007/s11030-016-9710-y
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Twenty ester-linked 1,4-disubstituted 1,2,3-triazoles having a furyl/thienyl moiety have been synthesized from heteroaryl prop-2-yn-1-yl carboxylate and aromatic azides via a Cu(I) catalyzed 1,3-dipolar cycloaddition. All the synthesized compounds were characterized by FTIR, H NMR, C NMR spectroscopy and HRMS. Synthesized triazoles were tested in vitro for antimicrobial evaluation against Gram-negative bacteria-Escherichia coli, Enterobacter aerogenes and Klebsiella pneumoniae; Gram-positive bacteria-Staphylococcus aureus and two fungal strains-Candida albicans and Aspergillus niger, reflecting moderate to good activity. The structure of compound 6f was also confirmed by X-ray crystallography (CCDC 1469326).
引用
收藏
页码:137 / 145
页数:9
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