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

Autor: Chia EW; Malaghan Institute of Medical Research, PO Box 7060, Wellington South, New Zealand., 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
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Nov 01; Vol. 16 (21), pp. 9432-42. Date of Electronic Publication: 2008 Sep 20.
DOI: 10.1016/j.bmc.2008.09.052
Abstrakt: 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.
Databáze: MEDLINE