含氧叔丁基三唑醇类化合物的合成及其体外抗真菌活性

Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(t-butyl)-3-(O-substituted)-2-propanols

目的设计合成含氧取代的叔丁基三唑醇类化合物并研究其体外抗真菌活性。方法以一氯频那酮为起始原料经多步反应合成目标化合物,化合物结构经1H-NMR谱、IR谱确证;选择8种真菌为实验菌株,按国际标准抗真菌敏感性实验方法测定体外抑菌活性。结果与结论合成了12个新化合物。所有目标化合物对8种真菌均具有一定的抑制作用。可以将现有的三唑醇类抗真菌药物结构中的2,4-二氟苯基替换成其他疏水性基团来设计抗真菌化合物。

Aim To study the antifungal activities of triazole derivatives bearing tert-butyl group and to compare their antifungal activities with that of the control drugs fluconazole and itraconazole. Methods Twelve target compounds were designed by the replacement of 2, 4-difluorophenyl group with tert-butyl moiety, The target compounds were confirmed by ^1H-NMR and IR. The MIC80 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 and conclusion 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. Other hydrophobic moieties besides 2, 4-difluorophenyl group can be introduced to design triazole compounds.