RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency

Bioorg Med Chem Lett. 2001 Mar 12;11(5):693-6. doi: 10.1016/s0960-894x(01)00034-8.

Abstract

Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in vitro profile than RPR200765A.

MeSH terms

  • Analysis of Variance
  • Animals
  • Area Under Curve
  • Arthritis, Rheumatoid / drug therapy
  • Cells, Cultured
  • Cytochrome P-450 Enzyme Inhibitors*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Lipopolysaccharides / pharmacology
  • Male
  • Mice
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Mitogen-Activated Protein Kinases / metabolism
  • Molecular Structure
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Random Allocation
  • Rats
  • Rats, Inbred Lew
  • Recombinant Proteins / metabolism
  • Tumor Necrosis Factor-alpha / metabolism
  • p38 Mitogen-Activated Protein Kinases

Substances

  • Cytochrome P-450 Enzyme Inhibitors
  • Enzyme Inhibitors
  • Lipopolysaccharides
  • Pyrimidines
  • RPR 203494
  • Recombinant Proteins
  • Tumor Necrosis Factor-alpha
  • Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases