title: Synthesis and anti-inflammatory effects of a series of novel 7-hydroxycoumarin derivatives.
abstract: A number of 7-hydroxycoumarins have been synthesised by Pechmann cyclisation using differently substituted resorcinols employing perchloric acid as the condensing agent. All the compounds have been characterised by analytical and spectroscopic methods. The anti-inflammatory properties were tested with LPS-induced inflammation in J774 macrophages. Expression of iNOS and COX-2 was determined by Western blot, NO by nitrite assay and IL-6 by ELISA analyses. Fifteen of the tested 7-hydroxycoumarins also inhibited IL-6 production but none of them had any major inhibitory effect on COX-2 expression.
authors.affiliation: Department of Chemistry, University of Eastern Finland, Joensuu Campus, PO Box 111, FIN-80101 Joensuu, Finland.
authors.forename: Juri M
authors.initials: JM
authors.lastname: Timonen
authors.forename: Riina M
authors.initials: RM
authors.lastname: Nieminen
authors.forename: Outi
authors.initials: O
authors.lastname: Sareila
authors.forename: Antonis
authors.initials: A
authors.lastname: Goulas
authors.forename: Lauri J
authors.initials: LJ
authors.lastname: Moilanen
authors.forename: Matti
authors.initials: M
authors.lastname: Haukka
authors.forename: Pirjo
authors.initials: P
authors.lastname: Vainiotalo
authors.forename: Eeva
authors.initials: E
authors.lastname: Moilanen
authors.forename: Paula H
authors.initials: PH
authors.lastname: Aulaskari
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015153:Blotting, Western; D002460:Cell Line; D018360:Crystallography, X-Ray; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004797:Enzyme-Linked Immunosorbent Assay; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D015850:Interleukin-6 / Q000096:biosynthesis; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D013329:Structure-Activity Relationship; D014468:Umbelliferones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000093242:Interleukin-6 Inhibitors
chemical_list: D000893:Anti-Inflammatory Agents; D051546:Cyclooxygenase 2; D015850:Interleukin-6; D008070:Lipopolysaccharides; D052247:Nitric Oxide Synthase Type II; D014468:Umbelliferones; D000093242:Interleukin-6 Inhibitors; C031477:7-hydroxycoumarin