Synthesis and anti-inflammatory structure–activity relationships of thiazine–quinoline–quinones: Inhibitors of the neutrophil respiratory burst in a model of acute gouty …

…, MV Berridge, L Larsen, NB Perry, CE Sansom…

Index: 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. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 21 p. 9432 - 9442

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Citation Number: 31

Abstract

Sixteen new thiazine–quinoline–quinones have been synthesised, plus one bicyclic analogue. These compounds inhibited neutrophil superoxide production in vitro with IC50s as low 60nM. 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 ...