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

Author(s): Behjat Pouramiri, Mohammad Mahdavi, Setareh Moghimi, Loghman Firoozpour, Hamid Nadri, Alireza Moradi, Esmat Tavakolinejad-Kermani, Ali Asadipour, Alireza Foroumadi

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 9 , 2016

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Graphical Abstract:


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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Article Details

Year: 2016
Published on: 02 October, 2016
Page: [897 - 902]
Pages: 6
DOI: 10.2174/1570180813666160610124637
Price: $65

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