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3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.

ABSTRACT: 3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration.

SUBMITTER: Pinard E

PROVIDER: S-EPMC4027785 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.

Pinard Emmanuel E Alberati Daniela D Alvarez-Sanchez Ruben R Brom Virginie V Burner Serge S Fischer Holger H Hauser Nicole N Kolczewski Sabine S Lengyel Judith J Mory Roland R Saladin Christian C Schulz-Gasch Tanja T Stalder Henri H

ACS medicinal chemistry letters 20140204 4

3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration. ...[more]

PMID: 24900853

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