Development of Orally Bioavailable Bicyclic Pyrazolones as Inhibitors of Tumor Necrosis Factor-α Production

Journal of Medicinal Chemistry
2004.0

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.

Knowledge Graph

Similar Paper

Development of Orally Bioavailable Bicyclic Pyrazolones as Inhibitors of Tumor Necrosis Factor-α Production
Journal of Medicinal Chemistry 2004.0
The development of new triazole based inhibitors of tumor necrosis factor-α (TNF-α) production
Bioorganic & Medicinal Chemistry Letters 2003.0
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors
Bioorganic & Medicinal Chemistry Letters 2004.0
The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Bioorganic & Medicinal Chemistry Letters 2005.0
Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-α (TNF-α) production
Bioorganic & Medicinal Chemistry Letters 2002.0
Synthesis and structure–activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-α
Bioorganic & Medicinal Chemistry Letters 2014.0
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide’s as an inhibitor of TNF-α production
Bioorganic & Medicinal Chemistry Letters 2018.0
From Imidazoles to Pyrimidines:  New Inhibitors of Cytokine Release
Journal of Medicinal Chemistry 2002.0
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: Part 1
Bioorganic & Medicinal Chemistry Letters 2009.0
Carbocyclic Nucleosides as Inhibitors of Human Tumor Necrosis Factor-α Production:  Effects of the Stereoisomers of (3-Hydroxycyclopentyl)adenines
Journal of Medicinal Chemistry 1996.0