Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds

T. G. Murali Dhar, Stephen T. Wrobleski, Shuqun Lin, Joseph A. Furch, David S. Nirschl, Yi Fan, Gordon Todderud, Sidney Pitt, Arthur M. Doweyko, John S. Sack, Arvind Mathur, Murray McKinnon, Joel C. Barrish, John H. Dodd, Gary L. Schieven, Katerina Leftheris

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38α MAP kinase with good cellular potency toward the inhibition of TNF-α production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38α is also disclosed.

Original languageEnglish (US)
Pages (from-to)5019-5024
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number18
DOIs
StatePublished - Sep 15 2007

All Science Journal Classification (ASJC) codes

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

Fingerprint

Dive into the research topics of 'Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds'. Together they form a unique fingerprint.

Cite this