Abstract
Eight new sulfonilamidothienopyrimidinone derivatives (1-8) were synthesized and evaluated for their antiinflammatory activity on the human keratinocyte line NCTC 2544. The potential anti-inflammatory activity of the derivatives (1-8) was evaluated by determining, through Western blot, the expression of cyclooxygenase (COX)-2, inducible NO synthase (iNOS), intercellular adhesion molecule-1 (ICAM-1), and the release of prostaglandins (PG)E2 and interleukin- 8 (IL-8). Moreover, through ELISA assay, the release of monocyte chemoattractant protein-1 (MCP-1), and interleukin- 8 (IL-8) was analyzed.
Our results demonstrated that the derivatives 3, 5, 6 and 8 act as excellent inhibitors of inflammatory markers: iNOS, COX-2, ICAM-1, MCP-1, and IL-8. These findings could be useful for the development of new drugs for the treatment of various inflammatory pathologies.
Keywords: Anti-inflammatory activity, cell cultures, COX-2 inhibitors, cytokine, immuno-modulatory membrane molecules, keratinocytes NCTC 2544, nitric oxide, pyrimidin-4-one system.
Medicinal Chemistry
Title:Synthesis and Biological Evaluation of Sulfonilamidothienopyrimidinone Derivatives as Novel Anti-inflammatory Agents
Volume: 10 Issue: 7
Author(s): Mariarita Barone, Andrea Santagati, Adriana C.E. Graziano, Cosimo G. Fortuna, Giuseppe Ronsisvalle and Venera Cardile
Affiliation:
Keywords: Anti-inflammatory activity, cell cultures, COX-2 inhibitors, cytokine, immuno-modulatory membrane molecules, keratinocytes NCTC 2544, nitric oxide, pyrimidin-4-one system.
Abstract: Eight new sulfonilamidothienopyrimidinone derivatives (1-8) were synthesized and evaluated for their antiinflammatory activity on the human keratinocyte line NCTC 2544. The potential anti-inflammatory activity of the derivatives (1-8) was evaluated by determining, through Western blot, the expression of cyclooxygenase (COX)-2, inducible NO synthase (iNOS), intercellular adhesion molecule-1 (ICAM-1), and the release of prostaglandins (PG)E2 and interleukin- 8 (IL-8). Moreover, through ELISA assay, the release of monocyte chemoattractant protein-1 (MCP-1), and interleukin- 8 (IL-8) was analyzed.
Our results demonstrated that the derivatives 3, 5, 6 and 8 act as excellent inhibitors of inflammatory markers: iNOS, COX-2, ICAM-1, MCP-1, and IL-8. These findings could be useful for the development of new drugs for the treatment of various inflammatory pathologies.
Export Options
About this article
Cite this article as:
Barone Mariarita, Santagati Andrea, Graziano C.E. Adriana, Fortuna G. Cosimo, Ronsisvalle Giuseppe and Cardile Venera, Synthesis and Biological Evaluation of Sulfonilamidothienopyrimidinone Derivatives as Novel Anti-inflammatory Agents, Medicinal Chemistry 2014; 10 (7) . https://dx.doi.org/10.2174/1573406410666140228152807
DOI https://dx.doi.org/10.2174/1573406410666140228152807 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
Related Articles
-
Current Evaluation of the Millennium Phytomedicine- Ginseng (II): Collected Chemical Entities, Modern Pharmacology, and Clinical Applications Emanated from Traditional Chinese Medicine
Current Medicinal Chemistry Preclinical Evaluation of Coronary Stents: Focus on Safety Issues
Current Vascular Pharmacology Strategies for Targeting IL-4 as a Novel Therapeutic Approach for the Treatment of Atopic Dermatitis
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Review of Dose-intense Platinum and/or Paclitaxel Containing Chemotherapy in Advanced and Recurrent Epithelial Ovarian Cancer
Current Pharmaceutical Design Fused 1,4-Dihydropyridines as Potential Calcium Modulatory Compounds
Mini-Reviews in Medicinal Chemistry Antiphospholipid Syndrome as a Neurological Disease
Current Rheumatology Reviews Functional and Molecular Changes of MSCs in Aging
Current Stem Cell Research & Therapy Antiphospholipid Antibody-Mediated Thrombotic Mechanisms in Antiphospholipid Syndrome: Towards Pathophysiology-Based Treatment
Current Pharmaceutical Design Synthesis, Preferentially Hypoxic Apoptosis and Anti-Angiogenic Activity of 3- Amino-1,2,4-Benzotriazine-1,4-Dioxide Bearing Alkyl Linkers with a 3-Amino-1,2,4- Benzotriazine-1-Oxide Moiety
Anti-Cancer Agents in Medicinal Chemistry Plant and Animal Steroids a New Hope to Search for Antiviral Agents
Current Medicinal Chemistry Novel Pentablock Copolymer Based Nanoparticles Containing Pazopanib: A Potential Therapy for Ocular Neovascularization
Recent Patents on Nanomedicine Epigenetic Therapies of Cancer
Current Cancer Therapy Reviews Natural Molecules as Talented Inhibitors of Nucleotide Pyrophosphatases/ Phosphodiesterases (PDEs)
Current Topics in Medicinal Chemistry Expedient and Green Synthesis of Some Novel 4-Thiazolidinones and New 2,4-Disubstituted Thiazoles with Tetrahydro Carbazole Pendant
Letters in Organic Chemistry Flavonoids Health Benefits and Their Molecular Mechanism
Mini-Reviews in Medicinal Chemistry Calorie Restriction and Dietary Restriction Mimetics: A Strategy for Improving Healthy Aging and Longevity
Current Pharmaceutical Design Protein Kinase C Isozymes: Memory Therapeutic Potential
Current Drug Targets - CNS & Neurological Disorders Recent Research Progress in Natural Bioactive Constituents against Lipid Metabolic Diseases
Current Topics in Medicinal Chemistry Ecto-Nucleotidase Inhibitors: Recent Developments in Drug Discovery
Mini-Reviews in Medicinal Chemistry Metabolism of Rhaponticin and Activities of its Metabolite, Rhapontigenin: A Review
Current Medicinal Chemistry