title: 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 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.
authors.forename: Mariarita
authors.initials: M
authors.lastname: Barone
authors.forename: Andrea
authors.initials: A
authors.lastname: Santagati
authors.forename: Adriana C E
authors.initials: AC
authors.lastname: Graziano
authors.forename: Cosimo G
authors.initials: CG
authors.lastname: Fortuna
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Ronsisvalle
authors.affiliation: Department of Biomedical (Physiology), University of Catania, V.le A. Doria 6-95125 Catania, Italy. cardile@unict.it.
authors.forename: Venera
authors.initials: V
authors.lastname: Cardile
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D051546:Cyclooxygenase 2 / Q000378:metabolism; D006801:Humans; D018799:Intercellular Adhesion Molecule-1 / Q000096:biosynthesis / Q000378:metabolism; D015394:Molecular Structure; D052247:Nitric Oxide Synthase Type II / Q000096:biosynthesis / Q000378:metabolism; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D019086:Bridged Bicyclo Compounds, Heterocyclic; D013449:Sulfonamides; D018799:Intercellular Adhesion Molecule-1; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2