AUTHOR=Hasanvand Zaman , Motahari Rasoul , Nadri Hamid , Moghimi Setareh , Foroumadi Roham , Ayati Adileh , Akbarzadeh Tahmineh , Bukhari Syed Nasir Abbas , Foroumadi Alireza TITLE=Novel 3-aminobenzofuran derivatives as multifunctional agents for the treatment of Alzheimer’s disease JOURNAL=Frontiers in Chemistry VOLUME=10 YEAR=2022 URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.882191 DOI=10.3389/fchem.2022.882191 ISSN=2296-2646 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.