摘要
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
Objective: To study the effect of fluconazole derivatives from introducing side chain containing sulfur atom on antifungal activity of fluconazole compounds. Methods: Fifteen title compounds were synthesized and confirmed by elementary analysis, 1H NMR and IR spectra. MICs of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards(NCCLS) using RPMI1640 test medium. Results: Among 15 title compounds,there were 13 new compounds.The results of preliminary antifungal test showed that all title compounds exhibited potent antifungal activities to a certain extent. The activity of compound 2 against Candida albicans was equal to that of fluconazole, its MIC 80 was 2 μg/ml. The activities of compound 7 and 10 against Candida albicans were 4 and 8 times as high as that of fluconazole respectively. Their MIC 80 were 0.5 and 0.25 μg/ml. Conclusion: Proper lipid/water distribition coefficient has more important influence on antifungal activities of title compounds than that of stereochemistry.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
2001年第9期871-874,共4页
Academic Journal of Second Military Medical University
