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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
曲秀艳1,2,夏东利1,2,李淑翠1*
0
(1.滨州医学院药理学教研室,烟台 2640032.胜利石油管理局滨南医院门诊药房,滨州 256606
*通信作者)
摘要:
[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
关键词:  合成  二唑  抗真菌药
DOI:
投稿时间:2013-04-01修订日期:2013-07-26
基金项目:
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
QU Xiu-yan1,2,XIA Dong-li1,2,LI Shu-cui1*
(1. Department of Pharmacology, Binzhou Medical College, Yantai 264003, Shandong, China2. Department of Pharmacy, Binnan Hospital of Shengli Petroleum Administration Bureau, Binzhou 256606, Shandong, China
*Corresponding author.)
Abstract:
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.
Key words:  synthesis  oxadiazoles  antifungal agents