Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.

Research paper by Masoumeh M Alipour, Mehdi M Khoobi, Alireza A Foroumadi, Hamid H Nadri, Alireza A Moradi, Amirhossein A Sakhteman, Mehdi M Ghandi, Abbas A Shafiee

Indexed on: 13 Nov '12Published on: 13 Nov '12Published in: Bioorganic & Medicinal Chemistry


A novel series of coumarin derivatives linked to benzyl pyridinium group were synthesized and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The enzyme inhibitory activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that compounds 3e, 3h, 3l, 3r and 3s have shown higher activity compared with donepezil hydrochloride as standard drug. Most of the compounds in these series had nanomolar range IC(50) in which compound 3r (IC(50) = 0.11 nM) was the most active compound against acetylcholinesterase enzyme.