Peer-reviewed veterinary case report
Discovery of imidazo[1,2-b]pyridazines as IKKβ inhibitors. Part 3: exploration of effective compounds in arthritis models.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2011
- Authors:
- Shimizu, Hiroki et al.
- Affiliation:
- R&D Division · Japan
- Species:
- rodent
Abstract
We have discovered imidazo[1,2-b]pyridazine derivatives that show suppressive activity of inflammation in arthritis models. We optimized the substructures of imidazo[1,2-b]pyridazine derivatives to combine potent IKKβ inhibitory activity, TNFα inhibitory activity in vivo and excellent pharmacokinetics. The compound we have acquired, which had both potent activities and good pharmacokinetic profiles based on improved physicochemical properties, demonstrated efficacy on collagen-induced arthritis models in mice and rats.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/21705219/