Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 21, Pages 9432-9442Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.09.052
Keywords
Thiazine-quinoline-quinones; Inflammation; Superoxide; Arthritis; Neutrophils
Funding
- TerraMarine Pharmaceuticals
- New Zealand Foundation for Research Science and Technology [CO1X0205]
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Sixteen new thiazine-quinoline-quinones have been synthesised, plus one bicyclic analogue. These compounds inhibited neutrophil superoxide production in vitro with IC(50)s as low 60 nM. Compounds with high in vitro anti-inflammatory activity were also tested in a mouse model of acute inflammation. The most active compounds inhibited both neutrophil infiltration and superoxide production at doses 2.5 mu mol/kg, highlighting their potential for development as novel NSAIDs. (C) 2008 Elsevier Ltd. All rights reserved.
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