Document Report Card
Basic Information
ID: ALA1142510
Journal: Bioorg Med Chem
Title: Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis.
Authors: Chia EW, Pearce AN, Berridge MV, Larsen L, Perry NB, Sansom CE, Godfrey CA, Hanton LR, Lu GL, Walton M, Denny WA, Webb VL, Copp BR, Harper JL.
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.
CiteXplore: 18835721