Bioorganic & Medicinal Chemistry Letters 2011-01-01

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

Vasudeva Naidu Sagi, Tianyu Liu, Xiaoying Lu, Tamas Bartfai, Edward Roberts, Vasudeva Naidu Sagi, Tianyu Liu, Xiaoying Lu, Tamas Bartfai, Edward Roberts, Vasudeva Naidu Sagi, Tianyu Liu, Xiaoying Lu, Tamas Bartfai, Edward Roberts

Index: Bioorg. Med. Chem. Lett. 21(23) , 7210-5, (2011)

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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.