The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38α MAP kinase inhibitor

John Hynes, Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, Gary L. Schieven, Kathleen M. Gillooly, David J. Shuster, Tracy L. Taylor, Xiao Xia Yang, Kim W. McIntyre, Murray McKinnon, Hongjian Zhang, Punit H. Marathe, Arthur M. Doweyko, Kevin Kish, Susan E. Kiefer, John S. Sack, John A. Newitt, Joel C. BarrishJohn Harold Dodd, Katerina Leftheris

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18 Scopus citations

Abstract

A novel structural class of p38α MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38α inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.

Original languageEnglish (US)
Pages (from-to)1762-1767
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number6
DOIs
StatePublished - Mar 15 2008

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Hynes, J., Wu, H., Pitt, S., Shen, D. R., Zhang, R., Schieven, G. L., Gillooly, K. M., Shuster, D. J., Taylor, T. L., Yang, X. X., McIntyre, K. W., McKinnon, M., Zhang, H., Marathe, P. H., Doweyko, A. M., Kish, K., Kiefer, S. E., Sack, J. S., Newitt, J. A., ... Leftheris, K. (2008). The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38α MAP kinase inhibitor. Bioorganic and Medicinal Chemistry Letters, 18(6), 1762-1767. https://doi.org/10.1016/j.bmcl.2008.02.031