3-甲基-1-苯基-2-吡唑啉-5-酮（依达拉奉）的构效关系
Structure-activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone).
作者信息
Watanabe Kazutoshi, Morinaka Yasuhiro, Iseki Katsuhiko, Watanabe Toshiaki, Yuki Satoshi, Nishi Hiroyoshi
机构信息
Research and Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan.
出版信息
Redox Rep. 2003;8(3):151-5. doi: 10.1179/135100003225001520.
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.
本文描述了一种新型自由基清除剂3-甲基-1-苯基-2-吡唑啉-5-酮（依达拉奉，1）作为一种有效的抗脂质过氧化抗氧化剂的发现。依达拉奉的构效关系表明，亲脂性取代基对于表现出其脂质过氧化抑制活性至关重要。体内研究表明，依达拉奉在短暂性脑缺血模型中显示出脑保护活性。
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