Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.
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作为 GalR2 亚微摩尔亲和配体的新型嘧啶衍生物的合成和生物学评价。
DOI：
10.1016/j.bmcl.2011.09.033
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发表时间：
2011
影响因子：
2.7
通讯作者：
Roberts,Edward
中科院分区：
文献类型：
--
作者：
Sagi,VasudevaNaidu;Liu,Tianyu;Lu,Xiaoying;Bartfai,Tamas;Roberts,Edward
GalR 1和GalR 2代表了治疗癫痫发作和癫痫的独特药理学靶点。合成了一系列新的2，4，6-三氨基嘧啶衍生物，并发现其对GalR 2具有亚微摩尔亲和力。对一系列2，4，6-三氨基嘧啶进行优化，发现了几种类似物，其IC 50值范围为0.3至1μM。
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.