5-Amino-pyrazoles as potent and selective p38α inhibitors

Jagabandhu Das, Robert V. Moquin, Alaric J. Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen Gillooly, Arthur M. Doweyko, John A. Newitt, John S. Sack, Hongjian Zhang, Susan E. Kiefer, Kevin Kish, Murray McKinnon, Joel C. Barrish, John H. Dodd, Gary L. Schieven, Katerina Leftheris

Research output: Contribution to journalArticlepeer-review

23 Scopus citations


The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on a 5-amino-pyrazole scaffold are described. These studies led to the identification of compound 2j as a potent and selective inhibitor of p38α MAP kinase with excellent cellular potency toward the inhibition of TNFα production. Compound 2j was highly efficacious in vivo in inhibiting TNFα production in an acute murine model of TNFα production. X-ray co-crystallography of a 5-amino-pyrazole analog 2f bound to unphosphorylated p38α is also disclosed.

Original languageEnglish (US)
Pages (from-to)6886-6889
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number23
StatePublished - Dec 1 2010

All Science Journal Classification (ASJC) codes

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


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