新型嘧啶衍生物的合成与生物评价作为 GalR2 的亚毫摩尔亲和配体。
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.
机构信息
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7210-5. doi: 10.1016/j.bmcl.2011.09.033. Epub 2011 Sep 25.
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.
摘要
GalR1 和 GalR2 是治疗癫痫和癫痫发作的独特药理学靶点。我们合成了一系列新型的 2,4,6-三氨基嘧啶衍生物，并发现它们对 GalR2 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，发现了几种具有 0.3 至 1 μM 范围内 IC50 值的类似物。
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