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Privileged Pharmacophore of FDA Approved Drugs in Combination with Chalcone Framework: A New Hope for Alzheimer's Treatment.
Combinatorial Chemistry & High Throughput Screening ( IF 1.6 ) Pub Date : 2020-10-31 , DOI: 10.2174/1386207323999200728122627
Bijo Mathew 1
Affiliation  

Multi-functional design of ligands emerged as a new drug design paradigm of Alzheimer’s disease (AD). Given the complexity of AD, the molecules showing dual inhibition of monoamine oxidase (MAO) and acetylcholinesterase (AChE) with neuroprotective properties could prevent the progressive neural degeneration effectively. Numerous studies documented that chalcone is a privileged structural framework for the inhibition of both MAO and AChE. The recent studies suggested that the development of chalcone candidates endowed with pharmacophores of FDA approved drugs may become an active molecules in the field of current AD research. The current perspective described the recent updates of chalcone moiety linked with the pharmacophores of flurbiprofen and rivastigmine hybrids as selective ChE/MAO-B inhibitors for the prophylactic agents for AD.



中文翻译:

FDA批准的药物与查尔酮骨架相结合的特权药理:阿尔茨海默氏症治疗的新希望。

配体的多功能设计作为阿尔茨海默氏病(AD)的一种新药设计范例出现了。鉴于AD的复杂性,具有神经保护特性的单胺氧化酶(MAO)和乙酰胆碱酯酶(AChE)具有双重抑制作用的分子可以有效地防止进行性神经变性。大量研究表明查尔酮是抑制MAO和AChE的特权结构框架。最近的研究表明,具有FDA批准药物药效基团的查耳酮候选物的开发可能成为当前AD研究领域中的活性分子。目前的观点描述了与氟比洛芬和利凡斯的明杂种的药效团相连的查耳酮部分的最新更新,其作为AD预防剂的选择性ChE / MAO-B抑制剂。

更新日期:2020-12-22
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