Abstract
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
Current Drug Discovery Technologies
Title: Anti-Inflammatory and Anti-Oxidant Activity of a New Class of Phenyl- Pyrazolone Derivatives
Volume: 3 Issue: 1
Author(s): C. Cusan, G. Altinier, S. Sosa, F. Sibilla, F. Bucar, A. Tubaro, M. Prato, G. Spalluto and T. Da Ros
Affiliation:
Keywords: Anti-inflammatory activity, anti-oxidant activity, phenidone, phenyl-pyrazolone derivative
Abstract: 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.
Export Options
About this article
Cite this article as:
Cusan C., Altinier G., Sosa S., Sibilla F., Bucar F., Tubaro A., Prato M., Spalluto G. and Ros Da T., Anti-Inflammatory and Anti-Oxidant Activity of a New Class of Phenyl- Pyrazolone Derivatives, Current Drug Discovery Technologies 2006; 3 (1) . https://dx.doi.org/10.2174/157016306776637573
DOI https://dx.doi.org/10.2174/157016306776637573 |
Print ISSN 1570-1638 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6220 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Editorial [Hot Topic: Why Apoptosis in Pediatric Disorders?]
Current Pediatric Reviews Patent Selections
Recent Patents on Anti-Cancer Drug Discovery AMPA Receptor Antagonist CFM-2 Decreases Survivin Expression in Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Stochastic Neighbor Embedding Algorithm and its Application in Molecular Biological Data
Current Bioinformatics Lipoprotein(a): Medical Treatment Options for an Elusive Molecule
Current Pharmaceutical Design Efficacy of Chemoembolization of Hepatocellular Carcinoma with Drug Eluting Beads
Recent Patents and Topics on Imaging (Discontinued) Coagulation and Cancer Therapy: The Potential of Natural Compounds
Current Genomics Kinase Regulation by Sulfur and Selenium Containing Compounds
Current Cancer Drug Targets Characterization of Molecular and Functional Alterations of Tumor Endothelial Cells to Design Anti-Angiogenic Strategies
Current Vascular Pharmacology HIF1A is Overexpressed in Medulloblastoma and its Inhibition Reduces Proliferation and Increases EPAS1 and ATG16L1 Methylation
Current Cancer Drug Targets Breast-Milk Characteristics Protecting Against Allergy
Endocrine, Metabolic & Immune Disorders - Drug Targets Reversible Covalent Binding of Neratinib to Human Serum Albumin In Vitro
Drug Metabolism Letters Muscarinic Activation Enhances the Anti-proliferative Effect of Paclitaxel in Murine Breast Tumor Cells
Anti-Cancer Agents in Medicinal Chemistry Dexamethasone Synergizes with Lenalidomide to Inhibit Multiple Myeloma Tumor Growth, But Reduces Lenalidomide-Induced Immunomodulation of T and NK Cell Function
Current Cancer Drug Targets Pharmacogenetics of Childhood Acute Lymphoblastic Leukemia
Current Pharmacogenomics Editorial [Hot Topic: Clinical Trials in ANCA Associated Vasculitis (Guest Editor: Chetan Mukhtyar)]
Current Immunology Reviews (Discontinued) Patents in Cancer Stem Cells
Recent Patents on Biomarkers Cancer Stem-Cells Patents in the Context of their Therapeutic Purposes: Exploring the Latest Trends (2011-2015)
Recent Patents on Regenerative Medicine Drug Metabolizing Enzymes and Transporters mRNA in Peripheral Blood Mononuclear Cells of Healthy Subjects: Biological Variations and Importance of Preanalytical Steps
Current Drug Metabolism Modulation of Protein-Protein Interactions as a Therapeutic Strategy for the Treatment of Neurodegenerative Tauopathies
Current Topics in Medicinal Chemistry