Synthesis of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-\[N-cyclopropyl-N-substituted amino\]-2-propanols and test of its antifungal activity
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Supported by National Natural Science Foundation of China(20772153) and Youth Initiation Program of Second Military Medical University.
Objective:To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain.Methods: Nine title compounds were synthesized and characterized by 1HNMR,MS spectra and element analysis.Eight fungi were used for in vitro anti-fungal test.Results: All of the title compounds showed antifungal activities of different extents,especially to the deep infection ones,and they had a MIC value < 0.125 μg/ml against Candida albicans,showing an anti-fungal activity 4 times higher than that of fluconzole and similar to that of totraconazaole.Conclusion: 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-\[N-cyclopropyl-N-(3,4-dichlorobenzyl) amino\]-2-propanols(6f) has a better activity ratio and is worth further studying.