Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378518 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
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-α 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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Adam Golebiowski, 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,