190967-03-4Relevant articles and documents
N-(5-Substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase
Beers, Scott A.,Malloy, Elizabeth A.,Wu, Wei,Wachter, Michael,Ansell, Justin,Singer, Monica,Steber, Michele,Barbone, Arminda,Kirchner, Thomas,Ritchie, David,Argentieri, Dennis
, p. 779 - 786 (2007/10/03)
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.