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Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.

Abstract：

:A group of novel quinoxalinone derivatives (4a-h) were prepared and investigated for their inhibitory activity against ALR2 and antioxidant activity. Most of them were found to be potent aldose reductase inhibitors with IC50 values ranging from 0.019 to 0.982 μM. The most active compound 2-(3-(4-hydroxyphenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid (4c) also had an excellent selectivity. In addition, a number of compounds showed strong antioxidant activity and the phenolic 3,5-dihydroxyl compound 4f with 7-chloro in the quinoxalinone core was most active in scavenging the DPPH radical and suppressing lipid peroxidation.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zou Y,Qin X,Hao X,Zhang W,Yang S,Yang Y,Han Z,Ma B,Zhu C

doi

10.1016/j.bmcl.2015.07.048

subject

Has Abstract

pub_date

2015-09-15 00:00:00

pages

3924-7

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00752-0

journal_volume

25

pub_type

杂志文章

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