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Peer-reviewed veterinary case report

Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2006
Authors:
Revesz, Laszlo et al.
Affiliation:
Novartis Institutes for BioMedical Research

Abstract

A test library with three novel p38alpha inhibitory scaffolds and a narrow set of substituents was prepared. Appropriate combination of substituent and scaffold generated potent p38alpha inhibitors, for example, pyrazolo[3,4-b]pyridine 9, pyrazolo[3,4-d]pyrimidine 18a and pyrazolo[3,4-b]pyrazine 23b with potent in vivo activity upon oral administration in animal models of rheumatoid arthritis.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/16249085/