简单双酰胺作为甘氨酸转运体1（GlyT1）强效抑制剂的设计、合成及构效关系
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
作者信息
Jolidon Synèse, Alberati Daniela, Dowle Adam, Fischer Holger, Hainzl Dominik, Narquizian Robert, Norcross Roger, Pinard Emmanuel
机构信息
F. Hoffmann-La Roche Ltd., Pharmaceutical Research Basel, Discovery Chemistry, CH-4070 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2008 Oct 15;18(20):5533-6. doi: 10.1016/j.bmcl.2008.09.005. Epub 2008 Sep 6.
Several novel classes of potent and small amide-type inhibitors of glycine transport (GlyT1) were developed through sequential simplification of a benzodiazepinone-lead structure identified from a high-throughput screening. The most potent compounds of these structurally simple classes show low nanomolar inhibition at the GlyT1 target.
通过对高通量筛选中鉴定出的苯并二氮杂卓酮先导结构进行逐步简化，开发出了几类新型的强效小分子酰胺型甘氨酸转运体（GlyT1）抑制剂。这些结构简单的类别中最有效的化合物对GlyT1靶点表现出低纳摩尔级别的抑制作用。
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