含查尔酮和罗丹宁乙酸结构化合物的合成及抗菌活性研究  

Synthesis and antibacterial activity of chalcone and rhodanine derivatives

作　　者：苗京[1] 宋明霞[1] 陈振华[1] 郑昌吉[1] 孙良鹏[1] 刘雪坤[1] 徐丽丽[1] 朴虎日[1] 

机构地区：[1]延边大学药学院长白山生物资源与功能分子教育部重点实验室,吉林延吉133002

出　　处：《延边大学医学学报》2013年第2期104-109,共6页Journal of Medical Science Yanbian University

基　　金：国家自然科学基金项目(20962021)

摘　　要：[目的]设计合成两类分别含有查尔酮和罗丹宁乙酸结构的化合物,并对其体外抗菌活性进行评价.[方法]以不同取代的苯乙酮和呋喃乙酸为起始原料,通过Vilsmeier-Haack反应获得目标化合物4a-o;以不同取代的氯苄和对羟基苯甲醛为起始原料,通过亲核取代反应和Knoevenagel反应获得目标化合物6a-l.[结果]合成了2个系列27个化合物,其结构经过核磁共振氢谱和质谱确认;体外抗菌实验结果表明,其中12个化合物表现出不同程度的抗菌活性.OBJECTIVE To design and synthesis two types of compounds containing rhodanine-3-acetic acid and chalcone structure, and to evaluate their antibacterial activities ~n vitro primarily. METHODS The target compounds 4a-o were synthesized with different substituted acetophenone and furan-2-carboxylic acid followed by the Vilsmeier-Haack strategy, and the target compounds 6a-1 were synthesized with different substituted benzyl chlorides and p-hydroxybenzaldehyde followed by the Knoevenagel strategy. RESULTS All the synthesized compounds were investigated by 1 H-NMR and MS. Pharmacological tests showed that twelve of them had antibacterial activities.

关 键 词：查尔酮 呋喃 罗丹宁乙酸 抗菌活性 

分 类 号：R914[医药卫生—药物化学]