2-\[(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基\]-5-(3,4,5-三甲氧基苯基)-1,3,4-二唑化合物的合成及抗真菌活性

摘要] 目的：寻找高效抗真菌化合物，探讨2-(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基]-5-(3,4,5-三甲氧基苯基)-1,3,4-噁二唑化合物的构效关系。方法：设计合成了20个2-(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基]-5-(3,4,5-三甲氧基苯基)-1,3,4-噁二唑化合物，用微量液基稀释法测定化合物对6种临床常见致病真菌:白念珠菌、新生隐球菌、热带念珠菌(Candida tropicalis)、近平滑念珠菌、红色毛癣菌、克鲁氏假丝酵母的体外抑菌活性。结果：体外抗真菌活性测试结果表明，所合成的目标化合物对所测菌株均具有一定的体外抗真菌活性。其中化合物8m, 8o对白色念珠菌的抑制活性约为氟康唑，酮康唑的3倍；化合物8a, 8e, 8k, 8l, 8n 和 8p对白色念珠菌的抑制活性也较氟康唑，酮康唑强。结论：所合成的化合物中，苯环上连有体积较小取代基的化合物抗真菌活性较好。 关键词] 合成；噁二唑；抗真菌活性

Design, synthesis and antifungal activities of 2-\[(1-substituted phenyl-1H-1,2,3-triazol- 4-yl)methylthio\]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole compounds

Objective: To search for the efficient antifungal activity compounds, and to discuss their structure-activity relationships. Methods: Twenty 2-(1-substituted phenyl-1H-1,2,3-triazol-4-yl)methylthio]-5-(3,4,5-trimethoxyphenyl)-1,3,4- oxadiazole compounds have been designed,and synthesized.. The broth microdilution method was performed to determine the minimal inhibitory concentration of all the compounds to six pathogenic fungi. Results: All the title compounds exhibited potent antifungal activities against the six pathogenic fungi to some extent. Conclusion: The activity of the compounds would be enhanced when the substituted groups on the benzene ring were smaller.