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ID: ALA1141693
Journal: Bioorg Med Chem Lett
Title: Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.
Authors: Pinard E, Alberati D, Borroni E, Fischer H, Hainzl D, Jolidon S, Moreau JL, Narquizian R, Nettekoven M, Norcross RD, Stalder H, Thomas AW.
Abstract: Screening of the Roche compound library led to the identification of the benzoylpiperazine 7 as a structurally novel GlyT1 inhibitor. The SAR which was developed in this series resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo efficacy after oral administration.
CiteXplore: 18752953