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Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha 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.
Afiliação
  • Clark MP; Health Care Research Center, Procter and Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, Ohio 45040, USA. clark.mp@pg.com
J Med Chem ; 47(11): 2724-7, 2004 May 20.
Article em En | MEDLINE | ID: mdl-15139749
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.
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Pirimidinas / Fator de Necrose Tumoral alfa Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2004 Tipo de documento: Article
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Pirimidinas / Fator de Necrose Tumoral alfa Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2004 Tipo de documento: Article