1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基)-3-(N-异丙基-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-difluoro-phenyl)-3-(N-isoproyl-N-substituted amino)-2-propanols

作　　者：魏宁[1] 张松伟[1] 但志刚[2] 柴晓云[2] 俞世冲[2] 吴秋业[2] 

机构地区：[1]中国人民解放军空军总医院,北京100036 [2]第二军医大学药学院有机化学教研室,上海200433

出　　处：《药学实践杂志》2009年第5期324-327,392,共5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:引入异丙基及取代氨基侧链结构,合成一系列目标化合物,所有化合物结构均经MS1、H-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15个目标化合物;所有化合物对所选真菌均表现出了一定的抑菌活性,其中化合物(6c),(6d),(6e),(6 f)和(6g)对除薰烟曲霉菌外的7种菌株都表现出了较好的抑菌活性。结论:取代氨基侧链结构的引入对目标化合物的抗菌活性有一定的影响,侧链为取代苄基活性较好,且取代苄基侧链越短,抑菌活性越好。Objective ： Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods ： A isopropyl and substituted amino group were introduced and a series of title compounds were synthesized. All of them were confirmed by MS, ^1H-NMR, et al. The antifungal activities were also evaluated against the eight common pathogenic fungi. Results ： Fifteen compounds were synthesized. All title compounds exhibited activity against fungi tested to some extent. Compounds （6c）, （6d）, （6e）, （6f） and （6g） exhibited strong antifangal activities against eight test fungi comparable to the control drug itraconazole except Aspergillus fumigatus. Conclusion：A benzyl moiety with a group of shorter length substituted on 4-position is required for high activity.

关 键 词：三唑醇衍生物 合成 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学]