Back to Search Start Over

Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ1–42 aggregation inhibitors and metal-chelating agents for Alzheimer's disease.

Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ1–42 aggregation inhibitors and metal-chelating agents for Alzheimer's disease.

Authors :
Xu, Ping
Zhang, Minkui
Sheng, Rong
Ma, Yongmin
Source :
European Journal of Medicinal Chemistry. Feb2017, Vol. 127, p174-186. 13p.
Publication Year :
2017

Abstract

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 β-amyloid peptide (Aβ) aggregation inhibitor. The in vitro biological evaluation revealed that most of these newly synthesized compounds exhibited good inhibitory activity against self-induced Aβ 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 IC 50 values for Aβ 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
127
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
121134002
Full Text :
https://doi.org/10.1016/j.ejmech.2016.12.045