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具有抗氧化和/或抗炎特性的多靶点导向化合物作为阿尔茨海默病的有效药物

Multi-Target Directed Compounds with Antioxidant and/or Anti- Inflammatory Properties as Potent Agents for Alzheimer's Disease.

作者信息

Papagiouvannis Georgios, Theodosis-Nobelos Panagiotis, Kourounakis Panos N, Rekka Eleni A

机构信息

Department of Pharmacy, School of Health Sciences, Frederick University, Nicosia, 1036, Cyprus.

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, 54124, Greece.

出版信息

Med Chem. 2021;17(10):1086-1103. doi: 10.2174/1573406416666201013161303.

Abstract

BACKGROUND

Alzheimer's Disease (AD) is one of the most common neurodegenerative disorders, characterized by memory deficits and cognitive impairment. Acetylcholinesterase inhibitors, NMDA receptor antagonists and nootropic agents are used clinically, but they have only symptomatic efficacy, attributed to the multifactorial character of AD. The multi-target directed compound approach is gaining attention and has been under investigation lately.

OBJECTIVE

This review selects several research articles, which describe the design, synthesis and biological evaluation of multi-targeting molecules combining antioxidant or/and anti-inflammatory properties. Compounds with these properties are expected to be beneficial in the treatment of AD.

METHODS

This review summarizes the pathobiochemistry of AD as well as the role of oxidative stress and inflammation in the progression of neurodegeneration. It presents novel compounds with antioxidant or/and anti-inflammatory activity that have been tested for their efficacy in neurodegenerative disorders.

RESULTS

Various researchers have taken advantage of the multi-targeting drug approach in order to design molecules which may be developed as useful agents for the treatment of neurodegeneration.

CONCLUSION

The multi-targeting compound approach is a developing therapeutic strategy for multifactorial diseases, such as AD, and can offer effective agents for their radical treatment.

摘要

背景

阿尔茨海默病(AD)是最常见的神经退行性疾病之一,其特征为记忆缺陷和认知障碍。临床上使用乙酰胆碱酯酶抑制剂、N-甲基-D-天冬氨酸(NMDA)受体拮抗剂和益智药,但由于AD的多因素特性,它们仅具有对症疗效。多靶点导向化合物方法正受到关注,且最近一直在研究中。

目的

本综述选取了几篇研究文章,这些文章描述了兼具抗氧化或/和抗炎特性的多靶点分子的设计、合成及生物学评价。预期具有这些特性的化合物对AD治疗有益。

方法

本综述总结了AD的病理生物化学以及氧化应激和炎症在神经退行性变进展中的作用。它展示了具有抗氧化或/和抗炎活性且已在神经退行性疾病中测试其疗效的新型化合物。

结果

众多研究人员利用多靶点药物方法来设计可能开发成为治疗神经退行性变有用药物的分子。

结论

多靶点化合物方法是针对AD等多因素疾病的一种正在发展的治疗策略,可为其根治提供有效药物。

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