title: Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.
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.
authors.affiliation: F. Hoffmann-La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH-4070 Basel, Switzerland. emmanuel.pinard@roche.com
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Pinard
authors.forename: Daniela
authors.initials: D
authors.lastname: Alberati
authors.forename: Edilio
authors.initials: E
authors.lastname: Borroni
authors.forename: Holger
authors.initials: H
authors.lastname: Fischer
authors.forename: Dominik
authors.initials: D
authors.lastname: Hainzl
authors.forename: Synèse
authors.initials: S
authors.lastname: Jolidon
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Moreau
authors.forename: Robert
authors.initials: R
authors.lastname: Narquizian
authors.forename: Matthias
authors.initials: M
authors.lastname: Nettekoven
authors.forename: Roger D
authors.initials: RD
authors.lastname: Norcross
authors.forename: Henri
authors.initials: H
authors.lastname: Stalder
authors.forename: Andrew W
authors.initials: AW
authors.lastname: Thomas