Synthesis and Biological Evaluation of Sulfonilamidothienopyrimidinone Derivatives as Novel Anti-inflammatory Agents

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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Synthesis and Biological Evaluation of Sulfonilamidothienopyrimidinone Derivatives as Novel Anti-inflammatory Agents

Author(s): Mariarita Barone, Andrea Santagati, Adriana C.E. Graziano, Cosimo G. Fortuna, Giuseppe Ronsisvalle and Venera Cardile

Affiliation: Department of Biomedical (Physiology), University of Catania, V.le A. Doria 6-95125 Catania, Italy.

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.

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Article Details

Volume: 10
Issue Number: 7
First Page: 700
Last Page: 710
Page Count: 11
DOI: 10.2174/1573406410666140228152807
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