Synthesis and analgesic activity of some 4,6-disubstituted-3(2H)-pyridazinone derivatives

Sukuroglu M. K. , Kupeli E., BANOĞLU E. , Unlu S., Yesilada E., Sahin M. F.

ARZNEIMITTELFORSCHUNG-DRUG RESEARCH, cilt.56, sa.5, ss.337-345, 2006 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 56 Konu: 5
  • Basım Tarihi: 2006
  • Doi Numarası: 10.1055/s-0031-1296731
  • Sayfa Sayıları: ss.337-345


A series of 6-morpholino-4-aryl-3(2H)-pyridazinone atkanoic 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 acetylsalicylic 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 (12ab, 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.