| Autor: |
Beers SA; R. W. Johnson Pharmaceutical Research Institute, Raritan NJ 08869, USA., Malloy EA, Wu W, Wachter M, Ansell J, Singer M, Steber M, Barbone A, Kirchner T, Ritchie D, Argentieri D |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 1997 Apr; Vol. 5 (4), pp. 779-86. |
| DOI: |
10.1016/s0968-0896(97)00025-4 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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