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 / 第二军医大学学报

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.