叔丁基三唑醇类衍生物的合成及其抗真菌活性

目的设计合成具有叔丁基结构的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、三氮唑为原料,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其体外抗真菌活性。结果设计合成了10个新化合物,所有化合物对8种真菌均有一定的抑制活性。结论立体化学因素对该类化合物的体外抑菌活性有较大影响。

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

Aim To study the antifungal activities of the triazole derivatives with the side chain containing tert-butyl 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,all and partly,respectively.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 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.Conclusion Stereochemistry has important influence on the antifungal activities of the target compounds.