37715-64-3Relevant academic research and scientific papers
2,5-disubstituted thiophenes: inhibitors of 5-lipoxygenase and inducible cyclooxygenase (COX-2) enzymes, composition and use
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, (2008/06/13)
2,5-Disubstituted thiophene derivatives, and more particularly, to 2-aryloxy-5-alkansulfonamido-thiophenes of the general formula: STR1 Wherein, R2 is CF3, C1 -C10 alkyl, or phenyl; X is O, S, or CH2
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.
