摘要
阿尔茨海默病是一种严重威胁老年人的神经退行性疾病,发病机制受到多种因素的影响。主要治疗药物是胆碱酯酶抑制剂,包括他克林、多奈哌齐、卡巴拉汀和加兰他敏等,它们能够抑制乙酰胆碱酯酶,提高乙酰胆碱水平,从而改善患者记忆认知功能。然而,他克林因其肝毒性退出了市场,为了降低其副作用,药物化学家们对他克林进行了改造和修饰。本文总结了近年他克林衍生物作为多靶点抗AD先导物的研究进展。
Alzheimer＇s disease is a progressive and degenerative neurological disorder among elderly people and many factors are involved in the disease progression. One therapy currently for AD is cholinesterase inhibitors which can raise acetylcholine levels in the cerebral cortex, such as tacrine, donepezil, rivastigmine, and galantamine. However, tacrine is limited in clinic use since it showed heptotoxicity. Thus, many efforts were carried out to modify tacrine to overcome its adverse effects. Tacrine-based derivatives as multi-target directed ligands for AD treatment was reviewed.
作者
郭卉艳
赵永梅
罗稳
GUO Hui-yan ZHAO Yong-nlei LUO Wen(Key Laboratory of Natural Medicine andlmmuno-Engineering, Henan University, Henan Kaifeng 475004 Pharmaceutical Engineering Department, Henan Vocational College of Applied Technology, Henan Kaifeng 475004, China)
出处
《广州化工》
CAS
2017年第15期17-20,共4页
GuangZhou Chemical Industry
基金
河南省教育厅重点科研项目(No.14A350008)
