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
-
Therapeutic Potential of Janus Kinase 3 (JAK3) Inhibitors
Current Pharmaceutical Design The Association between Tumor-associated Macrophages and Glioblastoma: A Potential Target for Therapy
Current Pharmaceutical Design Intravenous and Regional Paclitaxel Formulations
Current Medicinal Chemistry Development and Evaluation of Bioresponsive Tablets of a Selective COX-2 Inhibitor for Colonic Delivery
Drug Delivery Letters Molecular Pathways Associated with Aggressiveness of Papillary Thyroid Cancer
Current Genomics Tear Inflammatory Molecules in Contact Lens Wearers: A Literature Review
Current Medicinal Chemistry Anti-Platelet Treatment of Middle-Sized Abdominal Aortic Aneurysms
Current Vascular Pharmacology Magnetic Resonance Imaging of Short T2 Relaxation Components in Tissue Using Ultrashort Echo Time (UTE) Pulse Sequences
Current Medical Imaging The Basophil Granulocyte in Allergic Reactions: Experimental Models and their Use for the Identification of Drugs with Effects or Side Effects on Basophils
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Bisphosphonate Therapy in the Treatment of Multiple Myeloma
Current Pharmaceutical Design CCR2 Antagonists
Current Topics in Medicinal Chemistry Medicinal Agents and Metabolic Syndrome
Current Medicinal Chemistry Co-Morbidity and Self Medication in Schizophrenia: Involvement of Endogenous Morphine Signaling Mechanisms
Current Drug Targets Anti-obesity Agents: A Focused Review on the Structural Classification of Therapeutic Entities
Current Topics in Medicinal Chemistry Mesoionic Oxatriazoles (MOTA): NO-Donating Characteristics and Pharmacology
Current Pharmaceutical Design The Chemistry and Pharmacology of Genistein
The Natural Products Journal Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance
Mini-Reviews in Medicinal Chemistry Multivalent & Multifunctional Ligands to β-Amyloid
Current Pharmaceutical Design Cholesteryl Ester Transfer Protein (CETP) Inhibitors
Current Topics in Medicinal Chemistry Tissue Engineered Bone Grafts: Biological Requirements, Tissue Culture and Clinical Relevance
Current Stem Cell Research & Therapy