- Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis.
Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis.
Bioorganic & medicinal chemistry (2008-10-07)
Elizabeth W Chia, A Norrie Pearce, Michael V Berridge, Lesley Larsen, Nigel B Perry, Catherine E Sansom, Colette A Godfrey, Lyall R Hanton, Guo-Liang Leon Lu, Michaela Walton, William A Denny, Victoria L Webb, Brent R Copp, Jacquie L Harper
PMID18835721
摘要
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.