Abstract
AbstractA novel series of 2‐(4‐alkoxybenzylidine)‐2,3‐dihydro‐5,6‐dimethoxy‐1H‐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‐1H‐inden‐1‐one exhibited the most potent inhibitory activity with IC50 values of 0.3 and 7.4 μM for AChE and BuChE, respectively. This compound was found to be less toxic than donepezil.
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