Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.

@article{Pettus2010DiscoveryAE,
  title={Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.},
  author={Liping H Pettus and Ryan P Wurz and Shimin Xu and Brad Herberich and Bradley Henkle and Qiurong Liu and Helen J McBride and Sharon Mu and Matthew H Plant and Christiaan J. M. Saris and Lisa Sherman and Lu Min Wong and Samer Chmait and Matthew R Lee and Christopher J Mohr and Faye Hsieh and Andrew S Tasker},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 7},
  pages={2973-85}
}
The p38alpha mitogen-activated protein (MAP) kinase is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a variety of cytokines especially interleukin-1beta and tumor necrosis factor alpha. Thus, inhibitors of this enzyme are postulated to have significant therapeutic potential for the treatment of rheumatoid arthritis, inflammatory bowel disease, and Crohn… CONTINUE READING

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