| Literature DB >> 15837310 |
Adam Golebiowski1, Jennifer A Townes, Matthew J Laufersweiler, Todd A Brugel, Michael P Clark, Cynthia M Clark, Jane F Djung, Steven K Laughlin, Mark P Sabat, Roger G Bookland, John C VanRens, Biswanath De, Lily C Hsieh, Michael J Janusz, Richard L Walter, Mark E Webster, Marlene J Mekel.
Abstract
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo model of osteoarthritis. The X-ray crystal structure of a pyrazolone inhibitor cocrystallized with mutated p38 (mp38) is presented.Entities:
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Year: 2005 PMID： 15837310 DOI： 10.1016/j.bmcl.2005.03.007
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823