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 |
Externí odkaz: |
|