| Literature DB >> 15139749 |
Michael P Clark1, Steven K Laughlin, Matthew J Laufersweiler, Roger G Bookland, Todd A Brugel, Adam Golebiowski, Mark P Sabat, Jennifer A Townes, John C VanRens, Jane F Djung, Michael G Natchus, Biswanath De, Lily C Hsieh, Susan C Xu, Rick L Walter, Marlene J Mekel, Sandra A Heitmeyer, Kimberly K Brown, Karen Juergens, Yetunde O Taiwo, Michael J Janusz.
Abstract
2-Aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-alpha) inhibitors, which contain a novel bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-alpha production in monocytic cells. Secondary screening data are presented for the pyrimidinyl bicyclic pyrazolones. Several of these analogues showed good oral bioavailability in rat and efficacy in the rat iodoacetate in vivo model.Entities:
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Year: 2004 PMID： 15139749 DOI： 10.1021/jm049968m
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446