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

VN Sagi, T Liu, X Lu, T Bartfai, E Roberts

文献索引：Sagi, Vasudeva Naidu; Liu, Tianyu; Lu, Xiaoying; Bartfai, Tamas; Roberts, Edward Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 23 p. 7210 - 7215

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被引用次数: 7

摘要

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.