p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold

Bioorg Med Chem Lett. 2003 Jan 20;13(2):273-6. doi: 10.1016/s0960-894x(02)00876-4.

Abstract

A new class of p38 antagonists based on 3,4-dihydropyrido[3,2,-d]pyrimidine scaffold has been developed. These inhibitors exhibit unprecedented selectivity towards p38 over other very closely related kinases. Compounds 25, 33, and 34 were identified as benchmark analogues for follow-up studies. They show good potency for enzyme inhibition and excellent functional activity.

MeSH terms

  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Indicators and Reagents
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology*
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology*
  • Structure-Activity Relationship
  • p38 Mitogen-Activated Protein Kinases

Substances

  • Enzyme Inhibitors
  • Indicators and Reagents
  • Pyridines
  • Pyrimidinones
  • Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases