The development of monocyclic pyrazolone based cytokine synthesis inhibitors

Bioorganic & Medicinal Chemistry Letters
2005.0

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-alpha 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.

Knowledge Graph

Similar Paper

The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Bioorganic & Medicinal Chemistry Letters 2005.0
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors
Bioorganic & Medicinal Chemistry Letters 2004.0
Development of Orally Bioavailable Bicyclic Pyrazolones as Inhibitors of Tumor Necrosis Factor-α Production
Journal of Medicinal Chemistry 2004.0
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor
Bioorganic & Medicinal Chemistry Letters 2002.0
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-α production
Bioorganic & Medicinal Chemistry Letters 2006.0
Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents
Bioorganic & Medicinal Chemistry Letters 2015.0
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
From Imidazoles to Pyrimidines:  New Inhibitors of Cytokine Release
Journal of Medicinal Chemistry 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 biological evaluation of new pyrazolone–pyridazine conjugates as anti-inflammatory and analgesic agents
Bioorganic & Medicinal Chemistry 2014.0