Pyridopyrimidine analogues as novel adenosine kinase inhibitors

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2071-4. doi: 10.1016/s0960-894x(01)00375-4.

Abstract

A novel series of pyridopyrimidine analogues 9 was identified as potent adenosine kinase inhibitors based on the SAR and computational studies. Substitution of the C7 position of the pyridopyrimidino core with C2' substituted pyridino moiety increased the in vivo potency and enhanced oral bioavailability of these adenosine kinase inhibitors.

MeSH terms

  • Adenosine Kinase / antagonists & inhibitors*
  • Adenosine Kinase / metabolism
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Models, Molecular
  • Molecular Conformation
  • Morpholines / chemistry
  • Morpholines / pharmacology
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Morpholines
  • PD 173074
  • Pyrimidines
  • ABT 702
  • Adenosine Kinase