- N-(5-Substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase
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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.
- Beers, Scott A.,Malloy, Elizabeth A.,Wu, Wei,Wachter, Michael,Ansell, Justin,Singer, Monica,Steber, Michele,Barbone, Arminda,Kirchner, Thomas,Ritchie, David,Argentieri, Dennis
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p. 779 - 786
(2007/10/03)
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- Linear Free Energy ortho-Correlations in the Thiophene Series. Part 14. A Kinetic Study of the Benzenethiolate Debromination of Some 2-Bromo-5-nitro-3-X-thiophenes and 2-Bromo-3-nitro-5-X-thiophenes in Methanol.
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The study of the title reactions has furnished the following results: i) 3-substituted 2-bromo-5-nitrothiophenes show a good Hammett correlation for X = H, Br, CO2Me, SO2Me, Ac, CN,and NO2, ii) 3-methyl substituent causes a moderate activating effect (ks
- Noto, Renato,Frenna, Vincenzo,Consiglio, Giovanni,Spinelli, Domenico
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p. 2701 - 2710
(2007/10/02)
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