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Current Drug Discovery Technologies


ISSN (Print): 1570-1638
ISSN (Online): 1875-6220

Anti-Inflammatory and Anti-Oxidant Activity of a New Class of Phenyl- Pyrazolone Derivatives

Author(s): C. Cusan, G. Altinier, S. Sosa, F. Sibilla, F. Bucar, A. Tubaro, M. Prato, G. Spalluto and T. Da Ros

Volume 3, Issue 1, 2006

Page: [67 - 73] Pages: 7

DOI: 10.2174/157016306776637573

Price: $65


The anti-inflammatory activity of a new class of phenyl-pyrazolone derivatives, structurally related to phenidone, has been evaluated using the Croton oil ear test in mice as model of acute inflammation. Derivative 5h reduces the percentage of oedema similarly to indomethacin and more efficiently than phenylbutazone. The anti-inflammatory activity of these two reference drugs depends on their COX inhibition, but for the synthesized derivatives it has not been demonstrated a significant COX or LOX inhibition, as previously reported. While the anti-inflammatory activity of phenidone is correlated to its anti-oxidant properties, the redox potential of these compounds appears not decisive in the inflammatory process inhibition. In order to investigate the mechanism of action for these compounds, we quantified their anti-oxidant activity and the lipophilicity, and a relationship between the calculated logP and the percentage of oedema reduction was found. We hypothesize that the anti-inflammatory activity, recorded in vivo, could be related to lipophilic parameter of these compounds.

Keywords: Anti-inflammatory activity, anti-oxidant activity, phenidone, phenyl-pyrazolone derivative

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