Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591930 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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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Authors
Seema Bag, Sanjukta Ghosh, Rekha Tulsan, Abha Sood, Weihong Zhou, Christine Schifone, Michelle Foster, Harry III, Béla Török, Marianna Török,