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

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

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1
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States.

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.

PMID:
22018787
PMCID:
PMC3278223
DOI:
10.1016/j.bmcl.2011.09.033
[Indexed for MEDLINE]
Free PMC Article
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