503071-74-7Relevant academic research and scientific papers
Convergent synthesis of 2,3-bisarylpyrazolones through cyclization of bisacylated pyrazolidines and hydrazines
Brugel, Todd A.,Hudlicky, Tomas,Clark, Michael P.,Golebiowski, Adam,Sabat, Mark,Endoma, Mary Ann A.,Bui, Vu,Adams, David,Laufersweiler, Matthew J.,Maier, Jennifer A.,Bookland, Roger G.,De, Biswanath
, p. 3195 - 3198 (2007/10/03)
Cyclization of various bisacylated hydrazines and pyrazolidines using DBU or sodium hydride leads to the formation of various mono-, bi- and tricyclic pyrazolone scaffolds in 41-98% yield. The convergent nature by which the precyclization intermediates are constructed allows for rapid derivatization about the pyrazolone core.
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-α production
Clark, Michael P.,Laughlin, Steven K.,Laufersweiler, Matthew J.,Bookland, Roger G.,Brugel, Todd A.,Golebiowski, Adam,Sabat, Mark P.,Townes, Jennifer A.,VanRens, John C.,Djung, Jane F.,Natchus, Michael G.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Walter, Rick L.,Mekel, Marlene J.,Heitmeyer, Sandra A.,Brown, Kimberly K.,Juergens, Karen,Taiwo, Yetunde O.,Janusz, Michael J.
, p. 2724 - 2727 (2007/10/03)
2-Aryl-3-pyrimidinyl based tumor necrosis factor-α (TNF-α) inhibitors, which contain a novel bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-α production in monocytic cells. Secondary scre
