Peer-reviewed veterinary case report
The development of monocyclic pyrazolone based cytokine synthesis inhibitors.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2005
- Authors:
- Golebiowski, Adam et al.
- Affiliation:
- Procter and Gamble Pharmaceuticals · United States
- Species:
- rodent
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15837310/