Wu Qiuye

Design, synthesis, and antifungal activity of 3-substituted triazole derivatives.

Objective To study the in vitro antifungal activity of triazole alcohols by introduction of 1,2,3-triazole as the side chain.Methods Twenty-one novel triazole alcohol compounds were designed,synthesized,and characterized by 1 HNMR and MS spectra.The in vitro antifungal activities of the compounds were evaluated using eight kinds of pathogenic fungi.Results All the synthesized compounds exhibited certain antifungal activities.The MIC80value of compound7 1-(1 H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-[N,N-(1-substituted-benzyl-4-methylene-1 H-1,2,3-triazole)]against Candida albicans was 0.25μg/ml,with its activity being 4times that of fluconazole.The MIC80value of compoundⅥ1-(1 H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N,N-dipropargyl)-2-propanols against Candida albicans was 0.015 6μg/ml,with its activity being 64times that of fluconazole and 4times that of itraconazole.Conclusion The 1,2,3-triazole can be efficiently introduced by intermolecular 1,3-dipolar cycloaddition.Large side chains may be a disadvantage for improving the antifungal activity of the title compounds.

Synthesis of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-[N-cycloproyl-N-substituted amino]-2-propanols and test of its antifungal activity.

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.