Sarcosine based indandione hGlyT1 inhibitors

A series of sarcosine based indandione hGlyT1 inhibitors has been developed. Optimization of substitution around the indandione and sarcosine moieties has led to highly potent inhibitors at hGlyT1, which show selectivity over a number of other receptors.

Graphical abstractA series of indandione sarcosine hGlyT1 inhibitors has been developed, leading to very potent compounds, selective over a number of counterscreen receptors. Substitution around the indandione ring and the amino acid has been explored leading to compound 7c with an IC50 of 0.47 nM at hGlyT1.Figure optionsDownload full-size imageDownload as PowerPoint slide