全面分析基于加兰他敏的混合药物对阿尔茨海默病的治疗作用。

IF 3.2 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Yash Pal Singh, Sonima Prasad, Harish Kumar
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引用次数: 0

摘要

阿尔茨海默病(AD)是一种与年龄有关的渐进性慢性脑部神经退行性疾病,以丧失记忆力和其他认知功能为特征。阿尔茨海默病的确切病因仍在研究中,但神经递质乙酰胆碱(ACh)水平低下、淀粉样 beta(Aβ)以 Aβ 斑块形式聚集、tau 蛋白过度磷酸化形成神经纤维缠结(NFT)、氧化应激和金属离子失衡等因素是该病的主要特征。在 AD 的多种假说中,淀粉样蛋白-β(Aβ)假说和胆碱能假说是 AD 的主要靶向假说。一些研究人员假设,与胆碱能神经递质(乙酰胆碱)相关的主要事件是记忆丧失和认知障碍。由于该疾病的发病机制复杂,使用单一候选靶点进行长期治疗是徒劳的。因此,多靶点和多功能疗法应运而生。各研究团队正集中精力通过杂交技术解决多种疾病因素。因此,这种杂交方法已被应用于包括加兰他敏在内的所有核心支架。在本文中,我们试图全面概述有关加兰他敏(一种前瞻性 AChE 抑制剂)及其杂交类似物的最新进展,并将其作为治疗注意力缺失症的可能药物。此外,我们还提供了过去几十年中用于AD治疗的加兰他敏化合物的设计、合成和SAR分析。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A Comprehensive Analysis on Galantamine Based Hybrids for the Management of Alzheimer's Disease

Alzheimer's disease (AD) is a progressive chronic age-related neurodegenerative brain disorder characterized by the loss of memory and other cognitive functions. The exact etiology of AD is still under investigation, however several factors such as low level of neurotransmitter acetylcholine (ACh), aggregation of amyloid beta (Aβ) in the form of Aβ plaques, hyperphosphorylation of tau protein into neurofibrillary tangles (NFTs), oxidative stress, and metal ion imbalance are the major hallmarks of this disease. Of the multiple hypotheses for AD, the amyloid-β (Aβ) and cholinergic hypothesis are the main targeting hypotheses for AD. Some researchers hypothesized that the primary event associated with the cholinergic neurotransmitter (acetylcholine) is memory loss and cognitive impairment. Due to the disease's complicated pathogenesis, long-term therapy with a single target candidate is futile. As a result, multitargeted and multifunctional therapies have emerged. Various research teams are concentrating on addressing multiple disease factors through hybridization techniques. Consequently, this hybridization approach has been applied to all core scaffolds, including galantamine. In this article, we tried to provide a thorough overview of the most recent developments on galantamine, a prospective AChE inhibitor, and its hybrid analogs as possible therapeutic agents for treating AD. Furthermore, we also provided the design, synthesis, and SAR analysis of the galantamine-based compounds used in the last decades for the management of AD.

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来源期刊
Chemical Biology & Drug Design
Chemical Biology & Drug Design 医学-生化与分子生物学
CiteScore
5.10
自引率
3.30%
发文量
164
审稿时长
4.4 months
期刊介绍: Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.
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