Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 68, Issue -, Pages 291-300Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.07.045
Keywords
Alzheimer's disease; Coumarin; Tacrine; Cholinesterase inhibitor; Docking study
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Funding
- Research Council of Tehran University of Medical Sciences
- Iran National Elite Foundation (INEF)
- Iran National Science Foundation (INSF)
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Novel hybrid derivatives of two known scaffolds; tetrahydroaminoquinoline and coumarin were synthesized and evaluated for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities. By means of an efficient nanocatalyst, the reaction time for the syntheses of the target compounds was reduced. Subsequently, Ellman's modified method was used to evaluate the enzyme inhibitory activity of the synthesized structures. It was observed that most hybrid structures were moderate to potent inhibitors of AChE compared to Tacrine as the reference drug among which 7f with 4-fluorophenyl substituent was the most active compound (IC50 = 5 nM). (C) 2013 Elsevier Masson SAS. All rights reserved.
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