Abignente E, Arena F, Luraschi E, Saturnino C, Marmo E, Berrino L, Donnoli D
Dipartimento di Chimica Farmaceutica e Tossicologica, Facoltà di Farmacia Università di Napoli Federico II.
Farmaco. 1990 Oct;45(10):1075-87.
A group of ethyl esters of 2-phenylimidazo[1,2-b]pyridazine-3-carboxylic acids 3 were obtained by reaction in anhydrous ethanol of some substituted 3-aminopyridazines 1 with ethyl 2-benzoyl-2-bromoacetate 2. The acids 4 obtained via alkaline hydrolysis were tested in vivo for their antiinflammatory, analgesic and ulcerogenic actions and in vitro for their ability to inhibit the prostaglandin biosynthesis. Almost all of the new compounds showed high analgesic activity, whereas the activities exhibited in the other tests were sharply lower. These results are discussed in terms of mechanism of action.
通过一些取代的3 - 氨基哒嗪1与2 - 苯甲酰基 - 2 - 溴乙酸乙酯2在无水乙醇中反应，得到了一组2 - 苯基咪唑并[1,2 - b]哒嗪 - 3 - 羧酸的乙酯3。通过碱性水解得到的酸4在体内进行了抗炎、镇痛和致溃疡作用测试，在体外进行了抑制前列腺素生物合成能力的测试。几乎所有新化合物都表现出高镇痛活性，而在其他测试中表现出的活性则明显较低。根据作用机制对这些结果进行了讨论。
