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

Kazutoshi WatanabeResearch Laboratory I Pharmaceuticals Research Unit, Research & Development Division, Mitsubishi Pharma Corporation, Yokohama , Japan

Yasuhiro MorinakaMitsubishi Kagaku Medical Inc. Tokyo , Japan

Katsuhiko IsekiPharmaceutical Research Laboratories Toray Industries Inc., Kanagawa , Japan

Toshiaki WatanabeSales & Marketing Unit Integrated Marketing Unit, Marketing Department I, Mitsubishi Pharma Corporation, Osaka , Japan

Satoshi YukiResearch Laboratory II Pharmaceuticals Research Unit, Research & Development Division, Mitsubishi Pharma Corporation, Yokohama , Japan

Hiroyoshi NishiOffice of the President Mitsubishi Pharma Corporation, Osaka , Japan

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

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

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