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Preparation and antioxidant activity of alpha-pyridoin and its derivatives.

Abstract：

:Focusing on alpha-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) as the lead compound of the novel antioxidative enediol, we synthesized 5,5'- or 6,6'-bis-substituted derivatives of 1 from disubstituted pyridines. The antioxidant activity of 1 and its synthetic derivatives 2-7 was evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl radical) scavenging assay and inhibition of lipid peroxidation. In the DPPH assay, 1 exhibited an activity stronger than that of ascorbic acid, and 5,5'-dimethyl-(5) or 5,5'-dimethoxy-substituted derivatives (6) exhibited more potent activity than 1. The DPPH scavenging activities of alpha-pyridoins were correlated with their oxidation potential and thus the electron density of enediol. 5 and 6 effectively inhibited lipid peroxidation in the rat liver microsome/tert-butyl hydroperoxide system. Therefore, 5 and 6 serve as good candidates for a pharmacologically useful enediol antioxidant.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Hatanaka M,Takahashi K,Nakamura S,Mashino T

doi

10.1016/j.bmc.2005.07.065

subject

Has Abstract

pub_date

2005-12-15 00:00:00

pages

6763-70

issue

24

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00731-5

journal_volume

13

pub_type

杂志文章

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