Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 127, Issue -, Pages 174-186Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.12.045
Keywords
Resveratrol derivatives; 3-hydroxypyridin-4-one; Beta amyloid aggregation; Antioxidant; Metal chelator
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Funding
- Zhejiang provincial Natural Science Foundation of China [LY17H300005]
- Zhejiang Chinese Medical University [2015ZG15]
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A series of deferiprone-resveratrol hybrids have been designed and synthesized as multitarget-directed ligands (MTDLs) through merging the chelating moiety 3-hydroxypyridin-4-one into the structure of resveratrol, a natural antioxidant agent and beta-amyloid peptide (A beta) aggregation inhibitor. The in vitro biological evaluation revealed that most of these newly synthesized compounds exhibited good inhibitory activity against self-induced A beta(1-42) aggregation, excellent antioxidant activity and potent metal chelating capability. Compounds 3i and 4f were identified as the most promising MTDLs with triple functions, possessing micromolar IC50 values for A beta(1-42) aggregation inhibition, greater 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS(.+)) scavenging activity than Trolox and similar pFe(III) values to that of deferiprone. (C) 2016 Elsevier Masson SAS. All rights reserved.
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