Design,synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer’s disease |
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Authors: | Seema Bag Sanjukta Ghosh Rekha Tulsan Abha Sood Weihong Zhou Christine Schifone Michelle Foster Harry LeVine Béla Török Marianna Török |
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Institution: | 1. Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd, Boston MA 02125-3393, USA;2. Department of Molecular and Cellular Biochemistry, Chandler School of Medicine, Center on Aging, University of Kentucky, Lexington, KY 40536, USA |
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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. |
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Keywords: | Alzheimer’s disease Cholinesterase inhibition Amyloid beta Coumarins Chalcones |
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