1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代-2-丙醇类化合物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-substituted-2-propanol

作　　者：周宇 俞世冲[2] 王保刚[2] 闫永正[2] 吴秋业[2] 

机构地区：[1]解放军82医院药剂科,淮安223001 [2]第二军医大学药学院有机化学教研室,上海200433

出　　处：《第二军医大学学报》2011年第7期754-758,共5页Academic Journal of Second Military Medical University

基　　金：国家自然科学基金(20972188);上海市科委基础重点项目(09dZ1976700)~~

摘　　要：目的研究具有正丁基和三氮唑侧链结构的三唑醇类化合物的抗真菌活性。方法设计合成了16个1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代-2-丙醇类化合物,其结构都经过1HNMR和LC-MS确证。选择8种临床常见的真菌为实验菌株,进行体外抑菌活性测试。结果初步的体外抗真菌测试结果表明,所合成的化合物都有一定的抗真菌活性,其中化合物7b、7d、7 e和7 i对除薰烟曲霉菌外7种菌株的抑菌活性优于对照药氟康唑,与伊曲康唑相当。结论引入正丁基和三氮唑侧链的目标化合物都具有一定的抗真菌活性。Objective To study the antifungal activity of triazole alcohols by introduction of n-butyl and triazole as side chains.Methods A total of 16 compounds of 1-（1H-1,2,4-triazole-1-yl）-2-（2,4-difluorophenyl）-3-substituted-2-propanol were synthesized and characterized by 1HNMR and LC-MS.The in vitro antifungal activities of the compounds were determined by tests with 8 human pathogenic fungi.Results It was found that all the 16 title compounds exhibited antifungal activities,and compounds 7b,7d,7e and 7i had antifungal activities stronger than fluconazole,similar to itraconazole.Conclusion Introduction of n-butyl and triazole side chain can confer antifungal activities to the compounds.

关 键 词：合成 三唑类 抗真菌药 

分 类 号：R978.5[医药卫生—药品]