title: Synthesis and analgesic activity of some 4,6-disubstituted-3(2H)-pyridazinone derivatives.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Etiler, Ankara, Turkey.
authors.forename: Murat
authors.initials: M
authors.lastname: Süküroglu
authors.forename: Esra
authors.initials: E
authors.lastname: Küpeli
authors.forename: Erden
authors.initials: E
authors.lastname: Banoğlu
authors.forename: Serdar
authors.initials: S
authors.lastname: Unlü
authors.forename: Erdem
authors.initials: E
authors.lastname: Yeşilada
authors.forename: Mustafa Fethi
authors.initials: MF
authors.lastname: Sahin
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D016227:Benzoquinones; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000139:chemically induced
chemical_list: D000700:Analgesics; D016227:Benzoquinones; D007202:Indicators and Reagents; D011724:Pyridazines; C004532:quinone