N-(5-SUBSTITUTED) THIOPHENE-2-ALKYLSULFONAMIDES AS POTENT INHIBITORS OF 5-LIPOXYGENASE

Authors
BEERS SA MALLOY EA WU W WACHTER M ANSELL J SINGER M STEBER M BARBONE A KIRCHNER T RITCHIE D ARGENTIERI D
Citation
Sa. Beers et al., N-(5-SUBSTITUTED) THIOPHENE-2-ALKYLSULFONAMIDES AS POTENT INHIBITORS OF 5-LIPOXYGENASE, Bioorganic & medicinal chemistry, 5(4), 1997, pp. 779-786
Citations number
9
Categorie Soggetti
Biology,"Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry → ACNP
ISSN journal
09680896
Volume
5
Issue
4
Year of publication
1997
Pages
779 - 786
Database
ISI
SICI code
0968-0896(1997)5:4<779:NTAPIO>2.0.ZU;2-B
Abstract
Compound 4k N-[5-(4-fluoro) phenoxythien-2-yl] methanesulfonamide is r epresentative of a new class of potent inhibitors of 5-lipoxygenase (5 -LO). These versatile compounds exhibit dose-dependent inhibition of 5 -LO with IC(50)s ranging from 20-100 nM in the rat basophilic leukemia (RBL-1) cell homogenate assay and submicromolar IC,,s in both the RBL -1 and human peripheral blood leukocyte (PBL) whole cell assays. Compo und 4k also showed significant anti-inflammatory activity in the adjuv ant arthritic rat at an oral dose of 3 mg/kg. (C) 1997 Elsevier Scienc e Ltd.