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Synthesis and Antiacetylcholinesterase Activity Evaluation of New 2-Aryl Benzofuran Derivatives Publisher



Pouramiri B1 ; Mahdavi M2 ; Moghimi S2 ; Firoozpour L3 ; Nadri H4 ; Moradi A4 ; Tavakolinejadkermani E1 ; Asadipour A5 ; Foroumadi A2, 5
Authors
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Authors Affiliations
  1. 1. Department of Chemistry, Faculty of Science, Shahid Bahonar University of Kerman, Kerman, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
  5. 5. Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran

Source: Letters in Drug Design and Discovery Published:2016


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. © 2016 Bentham Science Publishers.
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