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

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

Volume: 13 Issue: 9

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

Affiliation:

Keywords: Benzofuran, acetylcholinesterase, N-bromosuccinimide (NBS), wittig reagent; alzheimer’s disease, 2-hydroxybenzyl alcohol.

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.

Cite this article as:

Pouramiri Behjat, Mahdavi Mohammad, Moghimi Setareh, Firoozpour Loghman, Nadri Hamid, Moradi Alireza, Tavakolinejad-Kermani Esmat, Asadipour Ali and Foroumadi Alireza, Synthesis and Antiacetylcholinesterase Activity Evaluation of New 2-aryl Benzofuran Derivatives, Letters in Drug Design & Discovery 2016; 13 (9) . https://dx.doi.org/10.2174/1570180813666160610124637

DOI https://dx.doi.org/10.2174/1570180813666160610124637	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X