Structure-activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone)

被引:55
作者
Watanabe, K
Morinaka, Y
Iseki, K
Watanabe, T
Yuki, S
Nishi, H
机构
[1] Mitsubishi Pharma Corp, Res Lab 1, Div Res & Dev, Aoba Ku, Yokohama, Kanagawa 2270033, Japan
[2] Mitsubishi Pharma Corp, Res Lab 2, Pharmaceut Res Unit, Div Res & Dev,Aoba Ku, Yokohama, Kanagawa 2270033, Japan
[3] Mitsubishi Kagaku Med Inc, Tokyo, Japan
[4] Toray Industries Ltd, Pharmaceut Res Labs, Kanagawa, Japan
[5] Mitsubishi Pharma Corp, Sales & Mkt Unit, Integrated Mkt Unit, Mkt Dept 1, Osaka, Japan
[6] Mitsubishi Pharma Corp, Off President, Osaka, Japan
关键词
D O I
10.1179/135100003225001520
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
This paper describes the discovery of a novel free radical scavenger, 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), as a potent antioxidant agent against lipid peroxidation. The structure-activity relationship of edaravone indicated that lipophilic substituents were essential to show its lipid peroxidation-inhibitory activity. In vivo studies revealed that edaravone showed brain-protective activity in a transient ischemia model.
引用
收藏
页码:151 / 155
页数:5
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