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Synthesis and anti-inflammatory effects of a series of novel 7-hydroxycoumarin derivatives.

TitleSynthesis and anti-inflammatory effects of a series of novel 7-hydroxycoumarin derivatives.
Publication TypeJournal Article
Year of Publication2011
AuthorsTimonen, J. M., Nieminen R. M., Sareila O., Goulas A., Moilanen L. J., Haukka M., Vainiotalo P., Moilanen E., & Aulaskari P. H.
JournalEur J Med Chem
Date Published2011 Sep
KeywordsAnimals, Anti-Inflammatory Agents, Blotting, Western, Cell Line, Crystallography, X-Ray, Cyclooxygenase 2, Enzyme-Linked Immunosorbent Assay, Inflammation, Interleukin-6, Lipopolysaccharides, Mice, Nitric Oxide Synthase Type II, Structure-Activity Relationship, Umbelliferones

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.

Alternate JournalEur J Med Chem
PubMed ID21680063


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