Synthesis and evaluation of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) as effective inhibitor of metal-induced Aβ aggregation and antioxidant.

Abstract:

:A series of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) at the 2-position were synthesized and evaluated for treatment of Alzheimer's disease. In vitro assays demonstrated that most of the target compounds exhibit significant inhibition of Cu(II)-induced Aβ1-42 aggregation, rapid H2O2 scavenging and glutathione peroxidise (GPx)-like catalytic activity. Among these molecules, compound 9a is the most potent peroxide scavenger that possesses the ability to scavenge most H2O2 within 200-220min and possesses GPx-like activity (v0=106.0μM·min(-1)), enabling modulation of metal-induced Aβ aggregation.

journal_name

Bioorg Med Chem

authors

Wang B,Wang Z,Chen H,Lu CJ,Li X

doi

10.1016/j.bmc.2016.08.017

subject

Has Abstract

pub_date

2016-10-01 00:00:00

pages

4741-4749

issue

19

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30624-1

journal_volume

24

pub_type

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