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Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity.

Abstract：

:To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-oxopyrido[3,2-b]pyrazin-4(3H)-yl) acetic acid (4k) was the most active with an IC50 value of 0.023 µM. Moreover, it was encouraging to find that some derivatives showed strong antioxidant activity, and among them, the phenolic 3,5-dihydroxyl compound 4l with 7-bromo in the core structure was proved to be the most potent, even comparable to that of the well-known antioxidant Trolox. Thus the results suggested success in the construction of potent and selective AKR1B1 inhibitors with antioxidant activity.

journal_name

J Enzyme Inhib Med Chem

journal_title

Journal of enzyme inhibition and medicinal chemistry

authors

Hao X,Qi G,Ma H,Zhu C,Han Z

doi

10.1080/14756366.2019.1643336

subject

Has Abstract

pub_date

2019-12-01 00:00:00

pages

1368-1372

issue

1

eissn

1475-6366

issn

1475-6374

journal_volume

34

pub_type

杂志文章

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