绕丹宁衍生物的合成方法和生物活性研究  

The Synthesis and Bioactivity of Rhodanine Derivatives

作　　者：全旺 安万凯[1] 李准 吴璐璐[1] 姜松[1] 潘振良[1] QUAN Wang;AN Wankai;LI Zhun;WU Lulu;JIANG Song;PAN Zhenliang(Henan Agricultural University,Faculty of Science,Zhengzhou 450002,China)

机构地区：[1]河南农业大学理学院,郑州450002

出　　处：《河南科学》2019年第3期361-368,共8页Henan Science

基　　金：国家自然科学基金(21702049);河南省高等学校重点科研项目(18A150006)

摘　　要：通过优化绕丹宁及其衍生物的合成路线,合成一系列绕丹宁衍生物,并研究其生物活性.以双羧甲基三硫代碳酸盐为原料,在水做溶剂的条件下与相应的胺反应,生成绕丹宁环,然后再与不同取代基的醛脱水缩合得到目标化合物.其结构经核磁共振谱等表征且同时进行抑菌活性测定.目标化合物5a,5c,5d对革兰氏阳性菌具有较好的抑菌活性,目标化合物5a,5b,5c,5d,5l,5n对革兰氏阴性菌具有较好的抑菌活性.该合成方法可用于合成绕丹宁类CFTR抑制剂.A series derivatives of rhodanine were synthesized by an optimized route and their biological activities were studied.As the raw material,bicarboxymethyl trithiocarbonate reacted with the corresponding amines in water.The rhodanine ring was formed and then dehydrated and condensed with different aldehydes.The target compounds were obtained.Their structures were confirmed by NMR spectrum.Their antibacterial activities were determined simultaneously.The compounds of 5a,5c and 5d showed good antibacterial activities to gram-positive bacteria,while the compounds of 5a,5b,5c,5d,5l and 5n showed good antibacterial activities to gram-negative bacteria.This method can be used to synthesize rhodanine CFTR inhibitors.

关 键 词：绕丹宁 合成 抑菌活性 

分 类 号：O69[理学—化学]