1092843-92-9Relevant articles and documents
Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: Inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis
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.
experimental part, p. 9432 - 9442 (2009/04/11)
Sixteen new thiazine-quinoline-quinones have been synthesised, plus one bicyclic analogue. These compounds inhibited neutrophil superoxide production in vitro with IC50s 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 μmol/kg, highlighting their potential for development as novel NSAIDs.