基于2′,4′-二氟联苯基的新型1,2,4-三氮唑类化合物的合成及其抗真菌活性  

Synthesis and antifungal activity of novel 1,2,4-triazole compounds containing 2′,4′-difluorobiphenyl moiety

作　　者：陈勇[1] 魏文博 段坤坤 方家宝 张尹超 杨占涛 CHEN Yong;WEI Wenbo;DUAN Kunkun;FANG Jiabao;ZHANG Yinchao;YANG Zhantao(Chemistry & Chemical Industry School,Anyang Normal Universitry, Anyang, Henan 45500)

机构地区：[1]安阳师范学院化学化工学院,河南安阳455000

出　　处：《华中师范大学学报（自然科学版）》2020年第6期982-989,997,共9页Journal of Central China Normal University：Natural Sciences

基　　金：河南省自然科学基金项目(182300410295);河南省高等学校重点科研项目计划(16A150049);河南省新型光电功能材料重点实验室资助.

摘　　要：依据药物分子设计原理,设计合成了以2′,4′-二氟代联苯基为分子骨架的新型1,2,4-三氮唑化合物.目标化合物分子结构经核磁共振氢谱(1H NMR)、碳谱(13C NMR)、高分辨质谱(HRMS-ESI)进行确证.测试了目标化合物的体外抗真菌活性,测试结果表明,目标化合物5d,5e,6a,6b,7c的抗真菌活性较好,化合物5d,6a对白色念珠菌的抑菌活性和酮康唑、氟康唑的抑菌活性相当,化合物5d,5e,6a,7c对红色毛癣菌的抑菌活性接近酮康唑,优于氟康唑.According to the principle of drug molecular design,novel 1,2,4-triazole compounds with 2′,4′-difluorobiphenyl as molecular framework were designed and synthesized.The molecular structure of the target compounds were confirmed by 1H NMR,13C NMR,and HMRS-ESI.The in vitro antifungal activity of the target compounds were tested.The test results showed that the antifungal activity of the target compounds 5d,5e,6a,6b,7c was better.The antifungal activity of compounds 5d,6a against candida albicans was comparable to that of ketoconazole and fluconazole.The antifungal activity of compounds 5d,5e,7c against Trichophyton rubrum was close to ketoconazole and superior to fluconazole.

关 键 词：2′ 4′-二氟联苯 1 2 4-三氮唑 抗真菌活性 合成 

分 类 号：O626[理学—有机化学]