Synthesis and the antifungal activities of 1-(1H-1,2,4-triazole-1-yl)-2-(t-butyl)-3-[(4-substituted benzyl)-piperazin-1-yl]-2-propanols

Aim To study the antifungal activity of the triazole derivatives bearing the side chain containing(t-butyl) and the 4-(substituted benzyl)-piperazin and to compare their activities to those of fluconazole and(itraconazole.)Methods According to the structure of fluconazole,thirteen title compounds were designed and synthesized.All of them were confirmed by()~1H-NMR and parts of them were confirmed by IR,MS spectra.The MIC_(80) of all the title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards(NCCLS) using the RPMI 1640 test medium.Results All of the title compounds were reported firstly.The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent.Ⅲ_7 was better than fluconazole in vitro.Conclusion The title compounds with t-butyl and piperazine substituents have antifungal activities.Electrical property and stereochemistry may be important to the antifungal activities for the title compounds in vitro.