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

Bioorg Med Chem. 2008 Nov 1;16(21):9432-42. doi: 10.1016/j.bmc.2008.09.052.

Elizabeth W Chia ¹, 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

Affiliations

Affiliation

1 Malaghan Institute of Medical Research, PO Box 7060, Wellington South, New Zealand.

PMID: 18835721 DOI: 10.1016/j.bmc.2008.09.052

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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