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

Sagi, Vasudeva Naidu; Liu, Tianyu; Lü, Xiaoying; Bartfai, Tamas; Roberts, Edward

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

2011

Sagi, Vasudeva Naidu | Liu, Tianyu | Lü, Xiaoying | Bartfai, Tamas | Roberts, Edward

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 1μM.

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