Synthesis and Antiacetylcholinesterase Activity Evaluation of New 2-aryl Benzofuran Derivatives

Starting from 2-hydroxybenzyl alcohol, a series of 2-arylbenzofurans have been synthesized and evaluated as acetylcholinesterase inhibitors at 23 mu M 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.