作者
Yaghoub Pourshojaei, Ardavan Abiri, Khalil Eskandari, Zahra Haghighijoo, Najmeh Edraki, Ali Asadipour
发表日期
2019/12/27
期刊
Scientific reports
卷号
9
期号
1
页码范围
19855
出版商
Nature Publishing Group UK
简介
Acetylcholinesterase (AChE) catalyzes the conversion of Aβ peptide to its aggregated form and the peripheral anionic site (PAS) of AChE is mainly involved in this phenomenon. Also catalytic active site (CAS) of donepezil stimulates the break-down of acetylcholine (ACh) and depletion of ACh in cholinergic synapses are well established in brains of patients with AD. In this study, a set of compounds bearing phenoxyethyl amines were synthesized and their inhibitory activity toward electric eel AChE (eeAChE) and equine butyrylcholinesterase (eqBuChE) were evaluated. Molecular dynamics (MD) was employed to record the binding interactions of best compounds against human cholinesterases (hAChE and hBuChE) as well as donepezil as reference drug. In vitro results revealed that compound 5c is capable of inhibiting eeAChE activity at IC50 of 0.50 µM while no inhibitory activity was found for eqBuChE for up …
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Y Pourshojaei, A Abiri, K Eskandari, Z Haghighijoo… - Scientific reports, 2019