Synthesis,characterization and preliminary screening of regioisomeric 1-(3-pyridazinyl)-3-arylpyrazole and 1-(3-pyridazinyl)-5-arylpyrazole derivatives towards cyclooxygenase inhibition |
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| Authors: | Serdar Ünlü Erden Banoglu Shigeru Ito Tokihiro Niiya Gökçen Eren Berna Ökçelik |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Etiler, Ankara, 06330, Turkey;2. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10, Surugadai, Kanda, Chiyoda-Ku, Tokyo, 101-0062, Japan;3. Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, 814-0180, Japan |
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| Abstract: | 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 μM 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. |
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| Keywords: | COX-1 COX-2 pyrazole pyridazine pyridazinone cyclooxygenase |
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