Premium
Design, Synthesis and Biological Assessment of Novel 2‐(4‐Alkoxybenzylidine)‐2,3‐dihydro‐5,6‐dimethoxy‐1 H ‐inden‐1‐one Derivatives as hAChE and hBuChE Enzyme Inhibitors
Author(s) -
Mozaffarnia Sakineh,
Parsaee Faeze,
Payami Elmira,
Karami Hosna,
Soltani Somaieh,
Rashidi MohammadReza,
TeimuriMofrad Reza
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201901973
Subject(s) - butyrylcholinesterase , acetylcholinesterase , aché , donepezil , enzyme , chemistry , piperidine , in vitro , stereochemistry , cholinesterase , biochemistry , pharmacology , biology , medicine , dementia , disease
A novel series of 2‐(4‐alkoxybenzylidine)‐2,3‐dihydro‐5,6‐dimethoxy‐1 H ‐inden‐1‐one derivatives were designed, synthesized and evaluated as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE) enzymes. The in vitro studies showed that some of these molecules exhibited a significant ability to inhibit AChE and BuChE. Among them, 2‐[4‐[2‐(piperidine‐1‐yl)ethoxy]benzylidine]‐2,3‐dihydro‐5,6‐dimethoxy‐1 H ‐inden‐1‐one exhibited the most potent inhibitory activity with IC 50 values of 0.3 and 7.4 μM for AChE and BuChE, respectively. This compound was found to be less toxic than donepezil.