Synthesis and the antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazine-1-yl]-2-propanols

Aim To study the effect of the fluconzole derivatives from introducing the side chain containing(4-substituted)-piperazine-1-yl on the antifungal activity of fluconzole compounds.Methods Thirteen title compounds were synthesized and confirmed by the elementary analysis, 1H-NMR and IR spectra.The MICs of all the title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards(NCCLS)using the RPMI1640 test medium.Results All of the title compounds were firstly reported.The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent.The activity of the eight compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro.Conclusion The lipid/water distribution coefficient and stereochemistry have important influence on the antifungal activities of the title compounds.