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ID: ALA1147752
Journal: Bioorg Med Chem Lett
Title: Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.
Authors: Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Neumann U, Rucklin G.
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.
CiteXplore: 16249085