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Synthesis, Biological Evaluation and Molecular Modelling of 2′-Hydroxychalcones as Acetylcholinesterase Inhibitors

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Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia
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Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia
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Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Molecules 2016, 21(7), 955; https://doi.org/10.3390/molecules21070955
Received: 16 March 2016 / Revised: 15 July 2016 / Accepted: 16 July 2016 / Published: 22 July 2016
(This article belongs to the Section Medicinal Chemistry)
A series of 2′-hydroxy- and 2′-hydroxy-4′,6′-dimethoxychalcones was synthesised and evaluated as inhibitors of human acetylcholinesterase (AChE). The majority of the compounds were found to show some activity, with the most active compounds having IC50 values of 40–85 µM. Higher activities were generally observed for compounds with methoxy substituents in the A ring and halogen substituents in the B ring. Kinetic studies on the most active compounds showed that they act as mixed-type inhibitors, in agreement with the results of molecular modelling studies, which suggested that they interact with residues in the peripheral anionic site and the gorge region of AChE. View Full-Text
Keywords: Alzheimer’s disease; acetylcholinesterase; chalcones; molecular modelling Alzheimer’s disease; acetylcholinesterase; chalcones; molecular modelling
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Sukumaran, S.D.; Chee, C.F.; Viswanathan, G.; Buckle, M.J.C.; Othman, R.; Abd. Rahman, N.; Chung, L.Y. Synthesis, Biological Evaluation and Molecular Modelling of 2′-Hydroxychalcones as Acetylcholinesterase Inhibitors. Molecules 2016, 21, 955.

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