Synthesis and antifungal activity of the novel azole compounds
10.3969/j.issn.1006-0111.2017.01.006
- VernacularTitle:新型氮唑类化合物的合成及抗真菌活性研究
- Author:
Xuefeng KE
1
;
Jingzhe LI
;
Ben FU
;
Liangjing LI
;
Xiaoyun CHAI
;
Qiuye WU
Author Information
1. 第二军医大学药学院有机化学教研室
- Keywords:
azole;
1,3,4-oxadiazole;
synthesis;
antifungal activity
- From:
Journal of Pharmaceutical Practice
2017;35(1):22-25,59
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize novel triazole antifungal derivatives with 1 ,3 ,4-oxadiazole side chain for the study of antifungal activities. Methods Fourteen title compounds were synthesized via acylation ,aminolysis reaction ,cy-clization ,nucleophilic substitution ,etc. All the compounds were characterized by 1 H NMR ,MS spectra. The in vitro antifun-gal activities were evaluated against six human pathogenic fungi through the micro-broth dilution method. Results The title compounds exhibited strong antifungal activities against all the tested fungi ,especially against Candida albicans. Compounds 10d ,10i , 10l , and 10n were found to be the most effective , with a minimum inhibitory concentration (MIC80 ) of 0.003 9 μg/ml .They are 16-fold more potent than ICZ ( MIC80 0.062 5 μg/ml) and 64-fold more potent than FCZ (MIC80 0.25 μg/ml) .Conclusion The 1 ,3 ,4-oxadiazole side chain could affect the antifungal activities. That could be due to the prop-er incorporation between the 1 ,3 ,4-oxadiazole substituted phenyl ring with the target enzyme.
