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Research Article

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

, , , , , & show all
Pages 351-361 | Received 11 Jul 2006, Accepted 24 Aug 2006, Published online: 04 Oct 2008
 

Abstract

In a search for novel compounds with analgesic and anti-inflammatory activity, a series of regioisomeric 1-(3-pyridazinyl)-3-arylpyrazole (5af, 6af) and 1-(3-pyridazinyl)-5-arylpyrazole (7af, 8af) 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.

Acknowledgements

The investigation was supported by a research grant from the SPO (2003K120470-01).

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