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-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 56 Sayı: 5
  • Basım Tarihi: 2006
  • Doi Numarası: 10.1055/s-0031-1296731
  • Dergi Adı: ARZNEIMITTELFORSCHUNG-DRUG RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.337-345
  • Anahtar Kelimeler: analgesics, arylpiperazine, 3(2H)-pyridazinones, analgesic activity, synthesis, AMIDE DERIVATIVES, ANTINOCICEPTIVE ACTIVITY, PYRIDAZINE, TRAZODONE, SERIES, ACID
  • Gazi Üniversitesi Adresli: Evet

Özet

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.