Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, Amrita Health Science Campus, Kochi-682 041, India.
Comb Chem High Throughput Screen. 2020;23(9):842-846. doi: 10.2174/1386207323999200728122627.
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.
多功能配体的设计是阿尔茨海默病（AD）的一种新的药物设计范例。鉴于 AD 的复杂性，具有双重抑制单胺氧化酶（MAO）和乙酰胆碱酯酶（AChE）以及神经保护特性的分子可以有效防止进行性神经变性。大量研究表明，查尔酮是抑制 MAO 和 AChE 的一种重要结构框架。最近的研究表明，开发具有 FDA 批准药物药效团的查尔酮候选物可能成为当前 AD 研究领域的活性分子。本综述描述了将氟比洛芬和利伐斯的明杂合药物药效团与查尔酮部分连接的最新研究进展，作为 AD 预防性药物的选择性 ChE/MAO-B 抑制剂。
