Synthesis of 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluoro-phenyl)-3-(N-cyclopropyl-N-substituted amino)-2-propanols and its antifungal activity
10.3724/SP.J.1008.2008.01380
- Author:
Xiao-Juan LU
1
Author Information
1. Department of Organic Chemistry
- Publication Type:Journal Article
- Keywords:
Antifungal agents;
Cyclopropyl;
Synthesis;
Triazole
- From:
Academic Journal of Second Military Medical University
2010;29(11):1380-1383
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain. Methods: Ten title compounds were synthesized and characterized by 1 HNMR,MS spectra and element analysis. The MICs of the compounds were determined by in vitro test in 8 fungus strains. Results: The title compounds exhibited potent antifungal activities against 8 strains,especially for the deep infection ones. Some compounds had MIC80 values less than 0.125 μg · ml-1 against Candida albicans, showing an activity 4 time higher than that of fluconzole. Conclusion: The title compounds with cyclopropyl and alky substituents have antifungal activities,and the antifungal activity decreases as the alkyl side chains getting longer.
