Vergelli Claudia, Giovannoni Maria Paola, Pieretti Stefano, Di Giannuario Amalia, Dal Piaz Vittorio, Biagini Pierfrancesco, Biancalani Claudio, Graziano Alessia, Cesari Nicoletta
Dipartimento di Scienze Farmaceutiche, via Ugo Schiff 6, Sesto Fiorentino, 50019 Firenze, Italy.
Bioorg Med Chem. 2007 Aug 15;15(16):5563-75. doi: 10.1016/j.bmc.2007.05.035. Epub 2007 May 18.
A series of 4-amino-5-vinyl-3(2H)-pyridazinones and analogues were synthesized and their antinociceptive effect was evaluated in the mouse abdominal constriction model. Several of the novel compounds showed ED(50) values in the range 6-20mg/kg/sc and demonstrated to be able to completely protect all the treated animals from the effect of the noxious stimulus at 30 mg/kg/sc. SAR studies confirmed the essential role played by an amino or substituted amino function at position 4 and by a vinyl group at position 5 of the diazine system.
合成了一系列4-氨基-5-乙烯基-3(2H)-哒嗪酮及其类似物，并在小鼠腹部收缩模型中评估了它们的镇痛作用。几种新型化合物的半数有效剂量（ED50）值在6-20mg/kg皮下注射范围内，并且证明在30mg/kg皮下注射时能够完全保护所有受试动物免受有害刺激的影响。构效关系研究证实了哒嗪系统4位的氨基或取代氨基官能团以及5位的乙烯基所起的重要作用。
