Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3041-4. doi: 10.1016/s0960-894x(03)00642-5.

Abstract

We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency, but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has potent whole cell AK inhibitory potency, analgesic activity and minimal reduction of locomotor activity.

MeSH terms

  • Adenosine Kinase / antagonists & inhibitors*
  • Analgesics / chemical synthesis*
  • Analgesics / pharmacology
  • Animals
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Hyperalgesia / drug therapy
  • Inhibitory Concentration 50
  • Motor Activity / drug effects*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Enzyme Inhibitors
  • Pyrimidines
  • Adenosine Kinase