鉴定 2-(4-吡啶基)噻吩并吡啶酮类化合物为 GSK-3β 抑制剂。
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.
机构信息
Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy.
出版信息
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4823-7. doi: 10.1016/j.bmcl.2011.06.050. Epub 2011 Jun 29.
PMID:21764580
Abstract
The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.
摘要
报道了一种新型的 2-(4-吡啶基)噻吩并[2,3-d]嘧啶酮 GSK-3β 抑制剂系列的发现。X 射线晶体学揭示了其结合模式，并能够对 SAR 进行合理化。还介绍了为提高细胞活性和预测 CNS 穿透性而对模板的初步优化。
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