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

Abstract: Eight new sulfonilamidothienopyrimidinone derivatives (1-8) were synthesized and evaluated for their antiinflammatoryactivity 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, inducibleNO 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 ofvarious inflammatory pathologies.

Eight new sulfonilamidothienopyrimidinone derivatives (1-8) were synthesized and evaluated for their anti-inflammatory 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)E-2 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.