Nakagawa Hidehiko, Ohyama Ryo, Kimata Ayako, Suzuki Takayoshi, Miyata Naoki
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1, Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
Bioorg Med Chem Lett. 2006 Dec 1;16(23):5939-42. doi: 10.1016/j.bmcl.2006.09.005. Epub 2006 Sep 25.
We synthesized various 3-methyl-1-phenyl-5-pyrazolone (edaravone) derivatives and evaluated their oxidation potential and hydroxyl radical scavenging activity. It was found 3-methyl-1-(pyridin-2-yl)-5-pyrazolone had a much higher ability to scavenge the radical than did edaravone itself. Its efficient radical scavenging activity was assumed to be due to the increase of its anion form, an active form, by a hydrogen-bonded intramolecular base.
我们合成了多种3-甲基-1-苯基-5-吡唑啉酮（依达拉奉）衍生物，并评估了它们的氧化电位和羟自由基清除活性。结果发现，3-甲基-1-（吡啶-2-基）-5-吡唑啉酮清除自由基的能力比依达拉奉本身高得多。其高效的自由基清除活性被认为是由于通过氢键分子内碱增加了其阴离子形式（一种活性形式）。
