4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action

Claudia Vergelli; Maria Paola Giovannoni; Stefano Pieretti; Amalia Di Giannuario; Vittorio Dal Piaz; Pierfrancesco Biagini; Claudio Biancalani; Alessia Graziano; Nicoletta Cesari

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4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action

机译：4-氨基-5-乙烯基-3（2H）-哒嗪酮和类似物作为有效的抗伤害药：合成，SAR和作用机理的初步研究

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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 6-20 mg/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.

机译：合成了一系列的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抗伤害作用。几种新型化合物的ED_（50）值在6-20 mg / kg / sc范围内，并证明能够完全保护所有处理的动物免受30 mg / kg / sc的有害刺激的影响。 SAR研究证实，二嗪系统第4位的氨基或取代的氨基官能团和第5位的乙烯基具有重要作用。

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来源
《Bioorganic and Medicinal Chemistry》 |2007年第16期|p.5563-5575|共13页
作者
Claudia Vergelli; Maria Paola Giovannoni; Stefano Pieretti; Amalia Di Giannuario; Vittorio Dal Piaz; Pierfrancesco Biagini; Claudio Biancalani; Alessia Graziano; Nicoletta Cesari;
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作者单位

Dipartimento di Scienze Farmaceutiche, via Ugo Schiff 6, Sesto Fiorentino, 50019 Firenze, Italy;

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正文语种 eng
中图分类药学;生物化学;
关键词
pain; antinociception; vinylpyridazinones; SARs;

机译：疼痛;伤害感受;乙烯基吡嗪酮;SARs;

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4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action

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