Starting from 2-hydroxybenzyl alcohol, a series of 2-arylbenzofurans have been synthesized
and evaluated as acetylcholinesterase inhibitors at 23 µM by using modified colorimetric Ellman’s
method. The reaction sequence was completed in four steps. All of the fourteen synthesized
products were obtained in excellent yields without the need to tedious work-up step. In the last step,
different derivatives were obtained by the substitution of bromine with five and six-membered cyclic
and acyclic amines. Among the synthesized compounds, the best activity was observed in 1-(4-
(Benzofuran-2-yl) benzyl)piperidine 5c with 74% activity compared to donepezil as a reference drug.
Keywords: Benzofuran, acetylcholinesterase, N-bromosuccinimide (NBS), wittig reagent; alzheimer’s disease, 2-hydroxybenzyl alcohol.
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