Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7210-5. doi: 10.1016/j.bmcl.2011.09.033. Epub 2011 Sep 25.

Abstract

GalR1 and GalR2 represent unique pharmacological targets for treatment of seizures and epilepsy. A novel series of 2,4,6-triaminopyrimidine derivatives were synthesized and found to have sub-micromolar affinity for GalR2. Optimization of a series of 2,4,6-triaminopyrimidines led to the discovery of several analogs with IC50 values ranging from 0.3 to 1 μM.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anticonvulsants* / chemical synthesis
  • Anticonvulsants* / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Ligands*
  • Molecular Structure
  • Protein Binding / drug effects
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology
  • Receptor, Galanin, Type 2 / chemistry*
  • Seizures

Substances

  • Anticonvulsants
  • Ligands
  • Pyrimidines
  • Receptor, Galanin, Type 2
  • 2,4,6-triaminopyrimidine