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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Anticonvulsants* / chemical synthesis
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Anticonvulsants* / pharmacology
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Humans
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Inhibitory Concentration 50
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Ligands*
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Molecular Structure
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Protein Binding / drug effects
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology
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Receptor, Galanin, Type 2 / chemistry*
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Seizures
Substances
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Anticonvulsants
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Ligands
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Pyrimidines
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Receptor, Galanin, Type 2
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2,4,6-triaminopyrimidine