title: Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.
abstract: 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.
authors.affiliation: School of Chemistry, University College of Science, University of Tehran, PO Box 14155-6455, Tehran, Iran.
authors.forename: Masoumeh
authors.initials: M
authors.lastname: Alipour
authors.forename: Mehdi
authors.initials: M
authors.lastname: Khoobi
authors.forename: Alireza
authors.initials: A
authors.lastname: Foroumadi
authors.forename: Hamid
authors.initials: H
authors.lastname: Nadri
authors.forename: Alireza
authors.initials: A
authors.lastname: Moradi
authors.forename: Amirhossein
authors.initials: A
authors.lastname: Sakhteman
authors.forename: Mehdi
authors.initials: M
authors.lastname: Ghandi
authors.forename: Abbas
authors.initials: A
authors.lastname: Shafiee
mesh_terms: D000818:Animals; D001665:Binding Sites; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D004593:Electrophorus / Q000378:metabolism; D008958:Models, Molecular; D011726:Pyridinium Compounds / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D003374:Coumarins; D011726:Pyridinium Compounds