Benzothiazole based inhibitors of p38α MAP kinase

Chunjian Liu, James Lin, Sidney Pitt, Rosemary F. Zhang, John S. Sack, Susan E. Kiefer, Kevin Kish, Arthur M. Doweyko, Hongjian Zhang, Punit H. Marathe, James Trzaskos, Murray Mckinnon, John Harold Dodd, Joel C. Barrish, Gary L. Schieven, Katerina Leftheris

Research output: Contribution to journalArticlepeer-review

49 Scopus citations

Abstract

Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38α MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system. The proposed binding mode of this new class of p38α inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38α enzyme.

Original languageEnglish (US)
Pages (from-to)1874-1879
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number6
DOIs
StatePublished - Mar 15 2008

All Science Journal Classification (ASJC) codes

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

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