Synthesis of novel sulfanilamide-derived 1,2,3-triazoles and their evaluation for antibacterial and antifungal activities

被引:346
|
作者
Wang, Xian-Long [1 ]
Wan, Kun [1 ]
Zhou, Cheng-He [1 ]
机构
[1] Southwest Univ, Lab Bioorgan & Med Chem, Sch Chem & Chem Engn, Chongqing 400715, Peoples R China
关键词
Sulfanilamide; 1,2,3-Triazole; Antibacterial; Antifungal; 1,3-Dipolar cycloaddition; ANTIMICROBIAL ACTIVITY; CARBONIC-ANHYDRASE; BIOLOGICAL EVALUATION; CLICK CHEMISTRY; INHIBITORS; SULFONAMIDES; PROPHYLAXIS; DERIVATIVES;
D O I
10.1016/j.ejmech.2010.07.031
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel sulfanilamide-derived 1,2,3-triazole compounds were synthesized in excellent yields via 1,3-dipolar cycloaddition and confirmed by MS. IR and NMR spectra as well as elemental analyses. All the compounds were screened in vitro for their antibacterial and antifungal activities Preliminary results indicated that some target compounds exhibited promising antibacterial potency Especially, 4-amino-N-((1-dodecyl-1H-1,2,3-triazol-4-yl)methyl) benzenesulfonamide. N-((1-(2,4-dichlorobenzyl)- 1H-1,2,3-triazol-4-yl)methyl)-4-aminobenzenesulfonamide and 4-amino-N-((1-(2,4-difluorobenzyl)- 1H-1,2,3-triazol-4-yl)methyl) benzenesulfonamide were found to be the most potent compounds against all the tested strains except for Candida albicans (ATCC76615) and Candida mycoderma. (C) 2010 Elsevier Masson SAS All rights reserved.
引用
收藏
页码:4631 / 4639
页数:9
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