Author/Authors :
Scott A. Beers، نويسنده , , Elizabeth A. Malloy، نويسنده , , Wei Wu، نويسنده , , Michael Wachter، نويسنده , , Justin Ansell، نويسنده , , Monica Singer، نويسنده , , Michele Steber، نويسنده , , Arminda Barbone، نويسنده , , Thomas Kirchner، نويسنده , , David Ritchie، نويسنده , , Dennis Argentieri، نويسنده ,
Abstract :
Compound 4k N-[5-(4-fluoro)phenoxythien-2-yl]methanesulfonamide is representative of a new class of potent inhibitors of 5-lipoxygenase (5-LO). These versatile compounds exhibit dose-dependent inhibition of 5-LO with IC50s ranging from 20–100 nM in the rat basophilic leukemia (RBL-1) cell homogenate assay and submicromolar IC50s in both the RBL-1 and human peripheral blood leukocyte (PBL) whole cell assays. Compound 4k also showed significant anti-inflammatory activity in the adjuvant arthritic rat at an oral dose of 3 mg/kg.
