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

Aim To study antifungal activity of the triazole derivatives bearing the side chain containing tert-butyl and 4-(4-alkyloxyphenyl)-piperazin-1-yl and to compare their antifungal activities with that of fluconazole and itraconazole.Methods According to the structure of fluconazole,ten target compounds were designed and synthesized.All of them were confirmed by()~1H-NMR and IR spectra respectively.The MIC_(80) of all the target compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS) using the RPMI-1640 test medium.Results All the target compounds were firstly reported.The results of the preliminary antifungal test show that all the target compounds exhibit potent antifungal activities to a certain extent.The activities of four target compounds are 4 times as high as that of fluconazole and equal to that of itraconazole against Candida albicans in vitro.Conclusion More hydrophobic groups can be introduced to design triazole compounds and stereochemistry have important influence on the antifungal activities of the target compounds.