Süküroglu Murat, Küpeli Esra, Banoğlu Erden, Unlü Serdar, Yeşilada Erdem, Sahin Mustafa Fethi
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Etiler, Ankara, Turkey.
Arzneimittelforschung. 2006;56(5):337-45. doi: 10.1055/s-0031-1296731.
A series of 6-morpholino-4-aryl-3(2H)-pyridazinone alkanoic acids, their ester and amide derivatives were prepared and tested for their in vivo analgesic activity by using the p-benzoquinone-induced writhing test. The analgesic activity of the compounds 6-morpholino-4-aryl-3(2H)-pyridazinone (6a-b) were comparable but little lower than that of acetyl-salicylic acid (CAS 50-78-2) as an analgesic agent. The 6-morpholino-4-aryl-3(2H)-pyridazinones having a propanoic acid (10a-b), ester (7a) and amides (12a-b, 12d and 12g) as side chains at the position 2 of the pyridazinone ring showed higher activity than the reference compound without gastric ulceration forming potential. All other compounds generally showed higher activity but caused gastric ulceration in the animals.
制备了一系列6-吗啉代-4-芳基-3(2H)-哒嗪酮链烷酸及其酯和酰胺衍生物，并通过对苯醌诱导的扭体试验测试了它们的体内镇痛活性。化合物6-吗啉代-4-芳基-3(2H)-哒嗪酮(6a - b) 的镇痛活性相当，但略低于作为镇痛剂的乙酰水杨酸（CAS 50-78-2）。在哒嗪酮环的2位具有丙酸(10a - b)、酯(7a) 和酰胺(12a - b、12d和12g) 作为侧链的6-吗啉代-4-芳基-3(2H)-哒嗪酮显示出比无形成胃溃疡可能性的参考化合物更高的活性。所有其他化合物通常显示出更高的活性，但在动物中引起了胃溃疡。
