Issue 5, 2014

Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease

Abstract

Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 μM; BuChE, IC50 = 8.04 μM; SI = 1.23), significant inhibition of Aβ42 aggregation (57.78%, at 20 μM) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 μM; MAO-B, IC50 = 12.19 μM), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy.

Graphical abstract: Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease

Supplementary files

Article information

Article type
Concise Article
Submitted
07 Dec 2013
Accepted
14 Feb 2014
First published
17 Feb 2014

Med. Chem. Commun., 2014,5, 609-616

Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease

L. Pan, X. Wang, S. Xie, S. Li and L. Kong, Med. Chem. Commun., 2014, 5, 609 DOI: 10.1039/C3MD00376K

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