基于他克林的多靶点乙酰胆碱酯酶抑制剂的研究进展

Development of the multi-target-directed acetylcholinesterase inhibitors based on tacrine

乙酰胆碱酯酶(acetylcholinesterase,AChE)是目前治疗阿尔采末病(Alzheimer’s disease,AD)的一个重要靶点。其中基于他克林的二联体(dimeric)和杂合体(hybrid)的研究得到广泛重视。设计思路正由同时结合AChE双位点提高抑制活性和选择性转变为针对AD多靶点定向作用的开发。该文综述了基于他克林的二联体或杂合体的抗AD研究进展及对其展望。

Acetylcholinesterase is an important target for anti- Alzheimer＇ s disease now. Much attention has been paid to the development Of tacrine dimeric or hybrid compounds. The design strategy is transforming merely interacting with the two binding sites of acetylcholinesterase to get more activity and selectivity into the multi-target-directed function for the treatment of Alzheimer＇ s disease. Herein,the tacrine dimeric or hybrid compounds development and the prospect for the treatment of AD have been reviewed.