摘要
阿尔茨海默病(Alzheimer’s disease,AD)作为具有不同相互关联和限制性病理途径的多因素综合征,是老龄人口中发病率最高的疾病之一。多靶向配体(multitarget-directed ligands,MTDLs)的发现和发展为神经退行性疾病,特别是AD的药物治疗开辟了一个很有前景的创新治疗方案。MTDLs合并2个或多个药效团于单个药物小分子中,较抗AD单一药效团分子更能起到改善药动学参数、减轻不良反应等效果。本文归纳总结了近年来多靶点抗AD小分子新型候选药物的创新设计与合成研究进展,为开发优效的抗AD药物分子提供理论依据。
Alzheimer’s disease(AD),as a multifactorial syndrome with several interconnected and deregulated pathological pathways,is one of the diseases with the highest incidence among the elderly population.The discovery and development of multitarget-directed ligands(MTDLs)have opened up a promising innovative drug therapy for neurodegenerative diseases,in particular for AD.Two or more pharmacophores are incorporated into a single drug small molecule of MTDLs,leading to a better pharmacokinetic profile and alleviated side effects.MTDLs are more helpful to treat AD than a single pharmacophore molecule.The innovative design and synthesis study of novel-type multi-targeted small-molecule anti-AD candidate drugs in recent years are summarized in this paper,providing theoretical basis for the development of effective anti-AD molecules.
作者
何敏
刘少静
秦蓓
HE Min;LIU Shao-jing;QIN Bei(Department of Pharmacy Xi'an Medical University,Xi'an 710021,China;Institute of Pharmacy,Xi'an Medical University,Xi’an 710021,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2021年第17期1584-1591,共8页
Chinese Journal of New Drugs
基金
陕西省重点研发计划项目(2021ZDLSF03-05)
西安市科技计划项目(2020KJRC0135)
西安市未央区科技计划项目(201930)
西安医学院药学省级重点学科建设项目(2016YXXK09)
西安医学院校级重点药学学科(西医发[2019]96号)。
关键词
阿尔茨海默病
多靶向配体
小分子
合成
Alzheimer’s disease
multitarget-directed ligands
small molecules
synthesis
