• DOI:10.1016/J.BMCL.2004.03.106
Corpus ID: 37147746

Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.

@article{Rvsz2004NovelPI,
  title={Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.},
  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 Gerard Rucklin},
  journal={Bioorganic & medicinal chemistry letters},
  year={2004},
  volume={14 13},
  pages={
          3595-9
        }
}

• L. Révész, E. Blum, +6 authors Gerard Rucklin
• Published 2004
• Chemistry, Medicine
• Bioorganic & medicinal chemistry letters

A library of trisubstituted oxazoles, thiazoles, imidazoles (1,2,4- and 2,4,5-substituted) and imidazo[1,2-b]pyridines was prepared and evaluated in vitro as p38alpha inhibitors and in vivo in several models of rheumatoid arthritis. Four structures--32, 37, 45 and 59--were identified as potent inhibitors of p38alpha with high efficacy in the LPS induced TNFalpha release model in the mouse, the adjuvant induced arthritis and the collagen induced arthritis in the rat with ED50s between 1.0 and 9… Expand

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