Luraschi E, Arena F, Sacchi A, Laneri S, Abignente E, D'Amico M, Berrino L, Rossi F
Dipartimento di Chimica Farmaceutica e Tossicologica, Facoltà di Farmacia, Università di Napoli Federico II.
Farmaco. 1995 May;50(5):349-54.
A series of imidazo[1,2-b]pyridazine-2-acetic esters, acids and amides was synthesized and tested for antiinflammatory, analgesic and ulcerogenic activities. The ethyl esters were prepared by cyclocondensation of some 3-aminopyridazines with ethyl 4-chloroacetoacetate, followed by hydrolysis or ammonolysis in order to obtain the corresponding acids and amides. The capacity of inhibiting the carrageenan-induced edema in the rat paw and the writhes induced by acetic acid in mice were evaluated, as well as the ulcerogenic action in rats. The acidic derivatives showed significant analgesic activity which is comparable to that found in other series of imidazo[1,2-b]pyridazine analogs previously examined.
合成了一系列咪唑并[1,2 - b]哒嗪 - 2 - 乙酸酯、酸和酰胺，并对其抗炎、镇痛和致溃疡活性进行了测试。通过一些3 - 氨基哒嗪与4 - 氯乙酰乙酸乙酯的环缩合反应制备乙酯，然后进行水解或氨解以获得相应的酸和酰胺。评估了其抑制大鼠足爪角叉菜胶诱导的水肿和小鼠乙酸诱导的扭体反应的能力，以及对大鼠的致溃疡作用。酸性衍生物显示出显著的镇痛活性，与先前研究的其他咪唑并[1,2 - b]哒嗪类似物系列中的活性相当。
