1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基)-3-(N-环己基-N-取代氨基)-2-丙醇的合成及抗真菌活性  

Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols

作　　者：吴玮峰[1] 杨志辉[2] 但志刚[1] 薛云云[1] 胡宏岗[1] 柴晓云[1] 俞世冲[1] 吴秋业[1] 

机构地区：[1]第二军医大学药学院有机化学教研室,上海200433 [2]空军总医院药学部,北京100142

出　　处：《药学实践杂志》2009年第4期266-269,共4页Journal of Pharmaceutical Practice

基　　金：国家自然科学基金资助项目(NO.20772153);上海市重点学科资助项目(NO.B906)

摘　　要：目的:以氟康唑为先导化合物,设计合成新的三唑醇类化合物,并研究其抗真菌活性。方法:引入环己基侧链结构,合成一系列目标化合物,所有化合物结构均经MS、1H-NMR等谱确证;选择8种真菌为实验菌株,测定其体外抗真菌活性。结果:合成了11个未见文献报道的目标化合物,部分化合物对所选真菌均表现出了一定的抑菌活性。结论:引入环己基对抗真菌活性影响较大。Objective ： Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods ： A cyclohexyl group introduced and a series title compounds synthesized All of them were confirmed by MS, 1 H-NMR, et al. The anti- fungal activities were also evaluated against the eight common pathogenic fungi. Results：Eleven title compounds were synthesized. Some of the title compounds exhibited activity against fungi tested to some extent. Conclusion ： A cyclohexyl group introduced to the side chain affected the antifungal activity.

关 键 词：三唑醇衍生物 合成 环己基 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学]