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目的 :研究不同含硫侧链的引入对三唑醇类化合物抗真菌活性的影响。 方法 :设计合成了 15个含硫侧链取代三唑醇类化合物 ,其中 13个为新化合物 ;选择了 8种真菌为实验菌株 ,进行体外抑菌活性测试。结果 :目标化合物对所选菌株均有一定的抑制活性 ,其中化合物 2对白色念珠菌的 MIC80 值为 2 μg/ m l,与氟康唑的活性相当 ;化合物 7和 10对白色念珠菌的MIC80 值为 0 .5和 0 .2 5 μg/ m l,分别为氟康唑活性的 4倍和 8倍。结论 :适当的脂水分配系数对该类化合物体外抑菌活性的影响可能大于立体化学因素的影响
Objective: To study the effect of different sulfur-containing side chains on the antifungal activity of triadimenol. Methods: Fifteen sulfur-containing side-chain substituted triazole compounds were designed and synthesized, of which 13 were new compounds. Eight kinds of fungi were selected as experimental strains to test the antimicrobial activity in vitro. Results: The target compounds exhibited certain inhibitory activity against selected strains. The MIC80 value of Candida albicans against compound 2 was 2 μg / ml, which was comparable to that of fluconazole. The MIC80 values of Candida albicans for compounds 7 and 10 0.5 and 0.52 μg / ml, respectively, four times and eight times the activity of fluconazole. Conclusion: The effect of proper lipid-water partition coefficient on the antibacterial activity of these compounds in vitro may be greater than that of the stereochemical factors