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: | Unlü Serdar Banoglu Erden Ito Shigeru Niiya Tokihiro Eren Gökçen Okçelik Berna Sahin Mustafa Fethi |
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Institution: | Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Etiler, Ankara 06330, Turkey. sunlu@gazi.edu.tr |
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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 microM 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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