607721-73-3Relevant articles and documents
The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Golebiowski, Adam,Townes, Jennifer A.,Laufersweiler, Matthew J.,Brugel, Todd A.,Clark, Michael P.,Clark, Cynthia M.,Djung, Jane F.,Laughlin, Steven K.,Sabat, Mark P.,Bookland, Roger G.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Janusz, Michael J.,Walter, Richard L.,Webster, Mark E.,Mekel, Marlene J.
, p. 2285 - 2289 (2007/10/03)
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.