含哌嗪环的三唑醇类化合物的合成及体外抗真菌活性

目的设计合成含哌嗪环侧链的三唑醇类化合物并研究其体外抗真菌活性。方法以2-氯-2′,4′-二氟苯乙酮为起始原料经多步反应合成目标化合物，化合物结构经IR、^1H-NMR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。结果设计合成了11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。结论多个目标化合物的抗真菌活性明显高于阳性对照药氟康唑，其中化合物11具有广谱、高活性的优点，其体外抗真菌活性与对照药伊曲康唑相当，有进一步研究开发的价值。

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

Aim To design and synthesis triazole derivatives with the side chain containing 4-substitued-piperazin-1-yl and to investigate their antifungal activities in vitro.Methods According to the structure of fluconazole,eleven target compounds were designed and synthesized.All of them were confirmed by()1H-NMR or 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 Eleven target compounds were firstly reported.The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent.Conclusion Most of the target compounds showed higher antifungal activities than that of fluconazole.Especially,compound 11 showed strong antifungal activity with broad antifungal spectrum and is chosen for further study.