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A review on flavonoid-based scaffolds as multi-target-directed ligands (MTDLs) for Alzheimer's disease
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2018-05-07 , DOI: 10.1016/j.ejmech.2018.05.004
Leili Jalili-Baleh , Elaheh Babaei , Shahin Abdpour , Syed Nasir Abbas Bukhari , Alireza Foroumadi , Ali Ramazani , Mohammad Sharifzadeh , Mohammad Abdollahi , Mehdi Khoobi

Alzheimer's disease (AD), the most common form of dementia, is a multifactorial neurodegenerative disease. The target enzymes inhibition including cholinesterase, beta-secretase, monoamine oxidase and inhibition of amyloid-β aggregation as well as oxidative stress and metal chelation play an important role in the pathogenesis of AD. Chroman-4-one scaffold with benzo-γ-pyrone network is a privileged structure in organic synthesis and drug design. A large number of research has been carried out on modified naturally occurring chromanone scaffolds and/or synthesized new analogues, to obtain effective drugs for AD management. The present review summarizes aspects related to the multi-target-directed ligands (MTDLs) strategy in enzyme targets modulation performed with natural and synthesized chroman-4-one-based structures to look at their potential in the management of multifactorial Alzheimer's disease.



中文翻译:

黄酮类支架作为阿尔茨海默氏病多靶标配体(MTDL)的综述。

痴呆症最常见的形式是阿尔茨海默氏病(AD),是一种多因素神经退行性疾病。靶酶的抑制作用包括胆碱酯酶,β-分泌酶,单胺氧化酶和淀粉样β-聚集的抑制以及氧化应激和金属螯合在AD的发病机理中起重要作用。具有苯并-γ-吡喃酮网络的Chroman-4-one支架是有机合成和药物设计中的优先结构。已经对修饰的天然存在的苯并二氢吡喃酮骨架和/或合成的新类似物进行了大量研究,以获得用于AD管理的有效药物。

更新日期:2018-05-07
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