期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 3, 页码 1254-1267出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm501484b
关键词
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资金
- National Natural Science Foundation of China [21272025]
- Research Fund for the Doctoral Program of Higher Education of China [20111101110042]
- Beijing Natural Science Foundation [7142096]
- Science and Technology Commission of Beijing (China) [Z131100004013003]
Quinoxalin-2(1H)-one based design and synthesis produced several series of aldose reductase (ALR2) inhibitor candidates. In particular, phenolic structure was installed in the compounds for the combination of antioxidant activity and strengthening the ability to fight against diabetic complications. Most of the series 6 showed potent and selective effects on ALR2 inhibition with IC50 values in the range of 0.032-0.468 mu M, and 2-(3-(2,4-dihydroxyphenyl)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid (6e) was the most active. More significantly, most of the series 8 revealed not only good activity in the ALR2 inhibition but also potent antioxidant activity, and 2-(3-(3-methoxy-4-hydroxystyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid (8d) was even as strong as the well-known antioxidant Trolox at a concentration of 100 mu M, verifying the C3 p-hydroxystyryl side chain as the key structure for alleviating oxidative stress. These results therefore suggest an achievement of multifunctional ALR2 inhibitors having both potency for ALR2 inhibition and as antioxidants.
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