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European Journal of Medicinal Chemistry 2011-Sep

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

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Juri M Timonen
Riina M Nieminen
Outi Sareila
Antonis Goulas
Lauri J Moilanen
Matti Haukka
Pirjo Vainiotalo
Eeva Moilanen
Paula H Aulaskari

Keywords

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.

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