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.