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

  title={Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.},
  author={L. R{\'e}v{\'e}sz and E. Blum and F. D. di Padova and T. Buhl and R. Feifel and H. Gram and P. Hiestand and U. Manning and U. Neumann and Gerard Rucklin},
  journal={Bioorganic & medicinal chemistry letters},
  volume={16 2},
  • L. Révész, E. Blum, +7 authors Gerard Rucklin
  • Published 2006
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 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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