Design, synthesis and structure–activity relationship of simple bis-amides as potent inhibitors of GlyT1

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.

Graphical abstractNovel classes of potent and small bis-amide type inhibitors of GlyT1 were developed through simplification of a benzodiazepinone-lead structure identified from high-throughput screening.Figure optionsDownload full-size imageDownload as PowerPoint slide