新型三唑类抗真菌药物的合成及其抑菌活性研究  

Synthesis and antifungal activities of new triazole compounds

作　　者：庞涛[1] 吴茂诚[2] 王潇屹[3] 

机构地区：[1]第二军医大学附属长征医院药学部,上海200003 [2]第二军医大学药学院有机化学教研室,上海200433 [3]上海海洋大学食品学院,上海201306

出　　处：《药学实践杂志》2013年第5期373-376,共4页Journal of Pharmaceutical Practice

基　　金：上海市重点学科资助项目(B906);上海科委基金资助项目(09dZ1976700);全军特殊环境重点研究实验室资助项目

摘　　要：目的设计合成新的三氮唑类化合物,并对其进行体外抑菌活性研究。方法以1,3-二氟苯为原料,运用Click反应合成一系列目标化合物;用微量液体稀释法检测目标化合物,测定其体外抗真菌活性。结果合成了12个目标化合物;所有化合物对所选真菌均表现出一定的抑菌活性。结论取代基的电子效应对化合物活性有影响,供电子基团比吸电子基团对活性提高更有利。Objective To design and synthesis novel triazole antifungal derivatives and study the antifungal activity. Methods All the target compounds were prepared from 1,3 - difluorobenzene via click reaction; The antibacterial activities of the title com- pounds were determined with broth dilution method. Results Twelve compounds were synthesized and characterized by 1H NMR and MS. All the title compounds exhibited potent antifungal activities against nearly all fungi tested. Conclusion The electronic effects of the substituents affected the activity of compounds, specifically the electron - donating groups.

关 键 词：三唑 CLICK反应 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学]