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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
21
Issue
23
Identifiers
DOI: 10.1016/j.bmcl.2011.09.033
Keywords
  • Galanin
  • G Protein-Coupled Receptor
  • Seizure
  • Binding Affinities
Disciplines
  • Biology
  • Pharmacology

Abstract

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.

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