Amide derivatives of [6-(5-methyl-3-phenylpyrazole-1-yl)-3(2H)pyridazinone-2-yl]acetic acids as potential a analgesic and anti-inflammatory compounds

BANOĞLU E., Akoglu C., Unlu S., Kupeli E., Yesilada E., Sahin E.

ARCHIV DER PHARMAZIE, cilt.337, sa.1, ss.7-14, 2004 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 337 Sayı: 1
  • Basım Tarihi: 2004
  • Doi Numarası: 10.1002/ardp.200200738
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.7-14
  • Anahtar Kelimeler: pyridazinone, analgesic, anti, inflammatory, COX-1, COX-2, DIFFERENTIAL INHIBITION, COX-2 INHIBITORS, CYCLOOXYGENASE-2, SELECTIVITY, DRUGS
  • Gazi Üniversitesi Adresli: Evet

Özet

In this study, amide derivatives of [6-(5-methyl-3-phenyl-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were synthesized and tested for their in vivo analgesic and anti-inflammatory activity by using the p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds 6a, 6d, 6e, 6g, 6 h and 6 m were more potent than that of aspirin as an analgesic and indomethacin as an anti-inflammatory drug, respectively. The other derivatives generally resulted in comparable activity to reference compounds. Inhibitor activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human whole blood assay and found that these derivatives did not exert their analgesic and anti-inflammatory activities. through COX inhibition and other mechanisms might be involved.