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Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis |
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| Authors: | Chia Elizabeth W Pearce A Norrie Berridge Michael V Larsen Lesley Perry Nigel B Sansom Catherine E Godfrey Colette A Hanton Lyall R Lu Guo-Liang Leon Walton Michaela Denny William A Webb Victoria L Copp Brent R Harper Jacquie L |
| Institution: | Malaghan Institute of Medical Research, PO Box 7060, Wellington South, New Zealand. |
| Abstract: | 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 micromol/kg, highlighting their potential for development as novel NSAIDs. |
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