摘要
目的:研究具有环丙基结构的三唑醇类化合物的抗真菌活性。方法:设计合成了10个三唑醇类新化合物,其结构通过1HNMR、MS和元素分析验证,选择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8种真菌特别是深部真菌均有一定的抑制活性,部分化合物对白念珠菌的MIC80值<0.125μg/ml,是氟康唑活性的4倍以上。结论:引入环丙基和烷基侧链的目标化合物都具有抗真菌活性,随着烷基侧链增长,目标化合物的活性降低。
Objective： To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain. Methods： Ten title compounds were synthesized and characterized by 1 HNMR,MS spectra and element analysis. The MICs of the compounds were determined by in vitro test in 8 fungus strains. Results： The title compounds exhibited potent antifungal activities against 8 strains,especially for the deep infection ones. Some compounds had MIC80 values less than 0. 125 μg · ml^-1 against Candida albicans, showing an activity 4 time higher than that of fluconzole. Conclusion： The title compounds with cyclopropyl and alky substituents have antifungal activities,and the antifungal activity decreases as the alkyl side chains getting longer.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
2008年第11期1380-1383,共4页
Academic Journal of Second Military Medical University
基金
国家自然科学基金(20772153)
第二军医大学青年启动基金~~
关键词
合成
三唑醇类
环丙基
抗真菌药
synthesis
triazole
cyclopropyl
antifungal agents
