N-(5-Substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase

DOI: 10.1016/S0968-0896(97)00025-4

Source and publish data:

Bioorganic and Medicinal Chemistry p. 779 - 786 (1997)

Update date:2022-08-03

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Authors:

Beers, Scott A.

Malloy, Elizabeth A.

Wu, Wei Wu, Wei

Wachter, Michael

Ansell, Justin

Singer, Monica

Steber, Michele

Barbone, Arminda

Kirchner, Thomas

Ritchie, David

Argentieri, Dennis

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Article abstract of DOI:10.1016/S0968-0896(97)00025-4

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.

Full text of DOI:10.1016/S0968-0896(97)00025-4

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