Structure-activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone).
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.
Watanabe
Kazutoshi
K
Research and Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan. Watanabe.Kazutoshi@mb.m-pharma.co.jp
Morinaka
Yasuhiro
Y
Iseki
Katsuhiko
K
Watanabe
Toshiaki
T
Yuki
Satoshi
S
Nishi
Hiroyoshi
H
D000818:Animals; D000983:Antipyrine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology*; D000077553:Edaravone; D016166:Free Radical Scavengers / Q000737:chemistry* / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D016166:Free Radical Scavengers; D000077553:Edaravone; D000983:Antipyrine