Peer-reviewed veterinary case report
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2004
- Authors:
- Revesz, Laszlo et al.
- Affiliation:
- Novartis Institutes for BioMedical Research
Abstract
Benzoylpyridines and benzophenones were synthesized and evaluated in vitro as p38alpha inhibitors and in vivo in several models of rheumatoid arthritis. Oral activity was found to depend upon substitution: 1,1-dimethylpropynylamine substituted benzophenone 10b (IC50: 14 nM) and pyridinoyl substituted benzimidazole 17b (IC50: 21 nM) showed highest efficacy and selectivity with ED50s of 9.5 and 8.6 mg/kg p.o. in CIA.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15177483/