氟康唑新衍生物的合成与体外抗真菌活性研究  

Synthesis and in vitro Antifungal Activity of Novel Fluconazole Derivatives

作　　者：谭文娟[1] 刘兴东[1] 杨帆[1] 胡馨月[1] 白国静[1] 朱伟伟[1] 孟庆国[1] 

机构地区：[1]烟台大学药学院,山东烟台264005

出　　处：《烟台大学学报（自然科学与工程版）》2013年第4期271-275,共5页Journal of Yantai University(Natural Science and Engineering Edition)

基　　金：国家自然科学基金资助项目(81072534)

摘　　要：基于前期计算机辅助药物研究结果,结合Lipinski类药规则,保留了氟康唑的2,4-二氟苯基、叔醇羟基和一个三唑环,合成了8个C-3连接尿嘧啶侧链的氟康唑新衍生物,并测定了其体外抗真菌活性.新衍生物结构经1H NMR、MS确证,初步体外抗真菌活性试验表明,化合物3b对新生隐球菌表现出一定的抗真菌活性.Based on our previous computer-aided drug design results and Lipinski＇s rules, eight new fluconazole derivatives containing uracil linked to C-3 are synthesized by retaining the difluorophenyl group, the hydroxyl group and the triazole ring of fluconazole and their in vitro antifungal activities are determined. The structures of flucon- azole derivatives are confirmed by X n NMR and MS. Preliminary in vitro antifungal activities bioassay shows that compound 3b exhibits moderate in vitro antifungal activities against C. neo.

关 键 词：氟康唑 衍生物 合成 体外抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学]