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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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 and ">Alireza Foroumadi

Volume 13, Issue 9, 2016

Page: [897 - 902] Pages: 6

DOI: 10.2174/1570180813666160610124637

Price: $65

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.

Graphical Abstract

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