多靶点抗Alzheimer病活性他克林-阿魏酸缀合物的合成与活性研究  

Synthesis and Activity of Multi-Targeted Tacrine-Ferulic Acid Compounds against Alzheimer's Disease

作　　者：付迎波 FU Yingbo(College of Life and Health Sciences,Northeastern University,Shenyang 110819,China)

机构地区：[1]东北大学生命科学与健康学院,辽宁沈阳110819

出　　处：《化学与生物工程》2019年第5期51-55,共5页Chemistry & Bioengineering

摘　　要：针对Alzheimer病多病因发病的特点,设计并合成了两种同时具有抗乙酰胆碱酯酶、抗Aβ_((1-42))蛋白氧化以及络合金属离子3种活性的抗Alzheimer病活性缀合物,其结构通过~1HNMR和MS确证。该化合物包含他克林、阿魏酸和氨基酸的结构,氨基酸连接在阿魏酸的羧基上以利于分子通过血脑屏障。活性测试表明,两种化合物都具有较好的乙酰胆碱酯酶抑制活性和Aβ_((1-42))自聚集抑制活性。According to the characteristic of complicated pathogenesis of Alzheimer′s disease,we designed and synthesized two compounds with acetylcholinesterase inhibitory activity,Aβ(1-42) self-aggregation inhibitory activity,and metal ion complexing activity against Alzheimer′s disease,and confirmed their structures by 1HNMR and MS.The compounds contain the structures of Tacrine,ferulic acid,and amino acid,and amino acid is connected to the carboxyl group of ferulic acid,which makes it easier for the molecular to pass blood brain barrier.Furthermore,activity experiments show that two compounds have good acetylcholinesterase inhibitory activity and Aβ(1-42) self-aggregation inhibitory activity.

关 键 词：ALZHEIMER病 他克林 阿魏酸 

分 类 号：R971[医药卫生—药品]