title: 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.
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Pinard
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Daniela
authors.initials: D
authors.lastname: Alberati
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Ruben
authors.initials: R
authors.lastname: Alvarez-Sanchez
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Virginie
authors.initials: V
authors.lastname: Brom
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Serge
authors.initials: S
authors.lastname: Burner
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Holger
authors.initials: H
authors.lastname: Fischer
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Nicole
authors.initials: N
authors.lastname: Hauser
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Sabine
authors.initials: S
authors.lastname: Kolczewski
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Judith
authors.initials: J
authors.lastname: Lengyel
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Roland
authors.initials: R
authors.lastname: Mory
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Christian
authors.initials: C
authors.lastname: Saladin
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Tanja
authors.initials: T
authors.lastname: Schulz-Gasch
authors.affiliation: Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
authors.forename: Henri
authors.initials: H
authors.lastname: Stalder
keywords: 3-amido-3-aryl-piperidines; GlyT1 inhibitor; SAR; Schizophrenia