Novel 3-Aminobenzofuran Derivatives As Multifunctional Agents for the Treatment of Alzheimer’S Disease Publisher



Hasanvand Z¹ ; Motahari R¹ ; Nadri H² ; Moghimi S³ ; Foroumadi R⁴ ; Ayati A³ ; Akbarzadeh T¹ ; Bukhari SNA⁵ ; Foroumadi A^{1, 3}
Source: Frontiers in Chemistry Published:2022

Abstract

A novel multifunctional series of 3-aminobenzofuran derivatives 5a-p were designed and synthesized as potent inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The target compounds 5a-p were prepared via a three-step reaction, starting from 2-hydroxy benzonitrile. In vitro anti-cholinesterase activity exhibited that most of the compounds had potent acetyl- and butyrylcholinesterase inhibitory activity. In particular, compound 5f containing 2-fluorobenzyl moiety showed the best inhibitory activity. Furthermore, this compound showed activity on self- and AChE-induced Aβ-aggregation and MTT assay against PC12 cells. The kinetic study revealed that compound 5f showed mixed-type inhibition on AChE. Based on these results, compound 5f can be considered as a novel multifunctional structural unit against Alzheimer’s disease. Copyright © 2022 Hasanvand, Motahari, Nadri, Moghimi, Foroumadi, Ayati, Akbarzadeh, Bukhari and Foroumadi.