期刊
MEDICINAL CHEMISTRY RESEARCH
卷 24, 期 1, 页码 182-196出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1123-9
关键词
1,2,3-Triazole; Glucoside; Antibacterial; Antifungal
资金
- National Natural Science Foundation of China [21172181, 21372186, 81450110094, 81350110523]
- Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- Specialized Research Fund for the Doctoral Program of Higher Education of China (SRFDP) [20110182110007]
A series of novel d-glucose-derived 1,2,3-triazoles have been synthesized in excellent yields via Cu(I)-catalyzed 1,3-dipolar cycloaddition by using methyl alpha-d-glucopyranoside as starting material. All the new compounds were confirmed by H-1 NMR, C-13 NMR, IR, MS, and HRMS spectra, and their antimicrobial activities were screened against Gram-Positive, Gram-Negative bacteria, and fungi. Bioactive assay manifested that some of the synthesized glucose-derived 1,2,3-triazoles exhibited good antibacterial and antifungal activities. Notably, compound 5k gave the most potent efficiency with MIC50 value of 6 A mu M against Candida albicans, which was nine-fold more active than the reference drug Fluconazole. It also exhibited good antibacterial activity against Escherichia coli with the MIC50 value of 10.8 A mu M compared to Chloramphenicol while the corresponding hydrochloride 4k revealed remarkable inhibitory against Bacillus subtilis with an MIC50 value of 11 A mu M.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据