Author:
Hasanvand Zaman,Motahari Rasoul,Nadri Hamid,Moghimi Setareh,Foroumadi Roham,Ayati Adileh,Akbarzadeh Tahmineh,Bukhari Syed Nasir Abbas,Foroumadi Alireza
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.
Funder
Tehran University of Medical Sciences and Health Services
Cited by
3 articles.
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