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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Sagi, Vasudeva Naidu¹  Liu, Tianyu¹  Lu, Xiaoying²  Bartfai, Tamas²  Roberts, Edward¹ 

[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Mol & Integrat Neurosci Dept, La Jolla, CA 92037 USA

关键词: Galanin;    G protein-coupled receptor;    Seizure;    Binding affinities;   

DOI  :  10.1016/j.bmcl.2011.09.033

来源: Elsevier

【 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 1 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

Free