1-（1H-1, 2, 4-三唑－1-基）－2-叔丁基－3-［（4-取代苄基）－哌嗪－1-基］－2-丙醇的合成及其抗真菌活性的研究

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 MIC80 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 compands were reported firstly. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. Ⅲ7 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.