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

Authors: Watanabe, Kazutoshi¹; Morinaka, Yasuhiro²; Iseki, Katsuhiko³; Watanabe, Toshiaki⁴; Yuki, Satoshi⁵; Nishi, Hiroyoshi⁶

Source: Redox Report, Volume 8, Number 3, June 2003 , pp. 151-155(5)

Publisher: Maney Publishing

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Abstract:

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.

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Document Type: Research Article

DOI: http://dx.doi.org/10.1179/135100003225001520

Affiliations: 1: Research Laboratory I, Pharmaceuticals Research Unit, Research & Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan 2: Mitsubishi Kagaku Medical Inc., Tokyo, Japan 3: Pharmaceutical Research Laboratories, Toray Industries Inc., Kanagawa, Japan 4: Sales & Marketing Unit, Integrated Marketing Unit, Marketing Department I, Mitsubishi Pharma Corporation, Osaka, Japan 5: Research Laboratory II, Pharmaceuticals Research Unit, Research & Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan 6: Office of the President, Mitsubishi Pharma Corporation, Osaka, Japan