title: Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
abstract: A series of heterocyclic sulfonamides have been developed which are potent and selective inhibitors of hGlyT1. SAR studies to optimise the in vitro and in vivo properties are described. Optimisation of the central scaffold resulted in cyclohexane sulfones 28 and 29, which have good PK properties and show promise for further development.
authors.affiliation: Department of Medicinal Chemistry, Merck Sharp and Dohme, Neuroscience Research Centre, Harlow, Essex, UK.
authors.forename: Joanne L
authors.initials: JL
authors.lastname: Thomson
authors.forename: Wesley P
authors.initials: WP
authors.lastname: Blackaby
authors.forename: Andrew S R
authors.initials: AS
authors.lastname: Jennings
authors.forename: Simon C
authors.initials: SC
authors.lastname: Goodacre
authors.forename: Andrew
authors.initials: A
authors.lastname: Pike
authors.forename: Steve
authors.initials: S
authors.lastname: Thomas
authors.forename: Terry A
authors.initials: TA
authors.lastname: Brown
authors.forename: Alison
authors.initials: A
authors.lastname: Smith
authors.forename: Gopalan
authors.initials: G
authors.lastname: Pillai
authors.forename: Leslie J
authors.initials: LJ
authors.lastname: Street
authors.forename: Richard T
authors.initials: RT
authors.lastname: Lewis