中国新药杂志

抗阿尔茨海默病小分子药物的设计与合成研究进展

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何敏 ¹^,² , 刘少静 ¹^,² , 秦蓓 ¹^,²

中国新药杂志 | 综述 2021,30(17): 1584-1591

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中国新药杂志 |综述 2021 , 30 (17) : 1584 -1591

抗阿尔茨海默病小分子药物的设计与合成研究进展

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何敏¹^,², 刘少静¹^,², 秦蓓¹^,²

作者信息

¹西安医学院药学院，西安　710021

²西安医学院药物研究所，西安　710021

通讯作者:

秦蓓，女，教授，主要从事生物医药材料合成与活性评价研究。联系电话：（029）86177536，E-mail：qinbei0526@163.com。

作者简介:

何敏，女，博士，讲师，主要从事活性小分子合成及性能评价。E-mail：hemlzu2010@163.com。

Advances in the design and synthesis of multi-target small molecules against Alzheimer's disease

Min HE¹^,², Shao-jing LIU¹^,², Bei QIN¹^,²

Affiliations

¹Department of Pharmacy, Xi'an Medical University, Xi'an 710021, China

²Institute of Pharmacy, Xi'an Medical University, Xi'an 710021, China

出版时间: 2021-09-15

文章导航

摘要

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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。

关键词

阿尔茨海默病 / 多靶向配体 / 小分子 / 合成

Abstract

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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.

Key words

Alzheimer's disease / multitarget-directed ligands / small molecules / synthesis

引用本文

何敏, 刘少静, 秦蓓. 抗阿尔茨海默病小分子药物的设计与合成研究进展. 中国新药杂志, 2021 , 30 (17) : 1584 -1591 .

Min HE, Shao-jing LIU, Bei QIN. Advances in the design and synthesis of multi-target small molecules against Alzheimer's disease[J]. Chinese Journal of New Drugs, 2021 , 30 (17) : 1584 -1591 .

基金

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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)

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2021年第30卷第17期

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首发时间：2026-10-28
出版时间：2021-09-15

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出版历史

录用日期：2021-03-03

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)

作者信息

¹西安医学院药学院，西安　710021

²西安医学院药物研究所，西安　710021

通讯作者:

秦蓓，女，教授，主要从事生物医药材料合成与活性评价研究。联系电话：（029）86177536，E-mail：qinbei0526@163.com。

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https://castjournals.cast.org.cn/joweb/zgxyzz/CN/1322180240902832627

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2种不同金属材料的力学参数

科 Family	属数 Number of genus	种数 Number of species	占总种数比例 Percentage of total species (%)	属 Genus	种数 Number of species	占总种数比例 Percentage of total species (%)
鹅膏菌科Amanitaceae	2	11	5.26	鹅膏菌属 Amanita	10	4.78
小菇科 Mycenaceae	2	12	5.74	丝盖伞属 Inocybe	5	2.39
多孔菌科 Polyporaceae	8	14	6.70	蜡蘑属 Laccaria	5	2.39
红菇科 Russulaceae	3	23	11.00	小皮伞属 Marasmius	6	2.87
				小菇属 Mycena	11	5.26
				光柄菇属 Pluteus	5	2.39
				红菇属 Russula	17	8.13
				栓菌属 Trametes	5	2.39

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