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Bioorg Med Chem Lett. 2013 May 1;23(9):2614-8. doi: 10.1016/j.bmcl.2013.02.103. Epub 2013 Mar 14.

Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.

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  • 1Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd, Boston, MA 02125-3393, USA.

Abstract

A series of compounds containing an α,β-unsaturated carbonyl moiety, such as chalcones and coumarins were designed, synthesized and tested in a variety of assays to assess their potential as anti-Alzheimer's disease (AD) agents. The investigations included the inhibition of cholinesterases (AChE, BuChE), the inhibition of amyloid beta (Aβ) self-assembly and the disassembly of preformed Aβ oligomers. Several compounds showed excellent potential as multifunctional compounds for AD. Docking studies for 16 that performed well in all the assays gave a clear interpretation of various interactions in the gorge of AChE. Based on the results, the long-chain coumarin scaffold appears to be a promising structural template for further AD drug development.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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