含硫的三唑类化合物的合成及抗真菌活性研究

Synthesis and antifungal activities of novel triazole derivatives containing sulfur atoms

目的设计合成含有二硫代甲酸酯侧链的新型三氮唑类化合物,并研究其体外抗真菌活性。方法通过与二硫化碳的加成及取代反应合成了9个新型三氮唑类化合物,其结构通过1 H NMR和MS确证,并选择8种真菌为实验菌株,对其体外抗真菌活性进行测试。结果所有化合物对实验菌株均有一定的抗菌活性,尤其对白色念珠菌活性较好,化合物6d对白假丝酵母菌的MIC80值<0.125μg/ml,是伊曲康唑的64倍。结论引入丙基、硫元素和取代苄基侧链对目标化合物的抗真菌活性影响较大;二硫代甲酸酯结构的引入有利于提高三唑类化合物的体外抗真菌活性。

Objective To design and synthesis novel triazole antifungal derivatives with dithiocarbamates side chain and study the antifungal activities. Methods Nine title compounds were synthesized and characterized hy 1 H NMR, MS spectra. The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi. Results The title compounds exhibited strong antifungal activities. Some compounds showed excellent activities against Candida albicans with the MIC80 values less than 0. 125 g/ml,6d was 64 times higher than that of Itraconazole. Conclusion The introduction of the propyl, sulphur and benzyl moiety to the side chain could affect the antifungal activities.