title: Synthesis of new indole derivatives structurally related to donepezil and their biological evaluation as acetylcholinesterase inhibitors.
abstract: New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent.
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Ismail
authors.forename: Mona M
authors.initials: MM
authors.lastname: Kamel
authors.forename: Lamia W
authors.initials: LW
authors.lastname: Mohamed
authors.forename: Samar I
authors.initials: SI
authors.lastname: Faggal
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D000077265:Donepezil; D007189:Indans / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008958:Models, Molecular; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D007189:Indans; D007211:Indoles; D018697:Nootropic Agents; D010880:Piperidines; D000077265:Donepezil; D000110:Acetylcholinesterase