Synthesis, characterization and preliminary screening of regioisomeric 1-(3-pyridazinyl)-3-arylpyrazole and 1-(3-pyridazinyl)-5-arylpyrazole derivatives towards cyclooxygenase inhibition

Unlu, Serdar; BANOĞLU, ERDEN; Ito, Shigeru; Niiya, Tokihiro; EREN, GÖKÇEN; Okcelik, Berna; Sahin, Mustafa

doi:10.1080/14756360601073468

Synthesis, characterization and preliminary screening of regioisomeric 1-(3-pyridazinyl)-3-arylpyrazole and 1-(3-pyridazinyl)-5-arylpyrazole derivatives towards cyclooxygenase inhibition

Atıf İçin Kopyala

Unlu S., BANOĞLU E., Ito S., Niiya T., EREN G., Okcelik B., ...Daha Fazla

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.22, sa.3, ss.351-361, 2007 (SCI-Expanded)

Yayın Türü: Makale / Tam Makale
Cilt numarası: 22 Sayı: 3
Basım Tarihi: 2007
Doi Numarası: 10.1080/14756360601073468
Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Sayfa Sayıları: ss.351-361
Gazi Üniversitesi Adresli: Evet

Özet

In a search for novel compounds with analgesic and anti-inflammatory activity, a series of regioisomeric 1-(3-pyridazinyl)-3-arylpyrazole (5a-f, 6a-f) and 1-(3-pyridazinyl)-5-arylpyrazole (7a-f, 8a-f) derivatives were synthesized. The structure of these regioisomers was confirmed by spectral techniques. The compounds were preliminarily screened at 8 mu M concentration for their inhibitory activity against cyclooxygenase enzymes, COX-1 and COX-2, using a human whole blood test. The tested derivatives showed inhibitory activity for both enzymes and are worthy of further investigation for developing better leads.