Design, synthesis, and antifungal activity of 3-substituted triazole derivatives / 第二军医大学学报

ABSTRACT

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 1HNMR 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 MIC 80 value of compound 7 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-[N,N-(1-substituted-benzyl-4-methylene-1H-1,2,3-triazole)] against Candida albicans was 0.25 μg/ml, with its activity being 4 times that of fluconazole. The MIC80 value of compound VI 1-(1H-1,2,4-triazole- 1-yl)-2-(2,4-difluorophenyl)-3-(N,N-dipropargyl)-2-propanols against Candida albicans was 0.0156μg/ml, with its activity being 64 times that of fluconazole and 4 times 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.