title: 1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.
abstract: High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonamides as selective GlyT-1 inhibitors. Structure-activity relationships of this novel series and optimisation of the initial hit that led to the identification of (2), a potent and selective GlyT-1 inhibitor, are also presented.
authors.affiliation: Discovery Medicinal Chemistry, GlaxoSmithKline, Harlow, Essex CM19 5AW, UK. shahzad.rahman-1@gsk.com
authors.forename: Shahzad S
authors.initials: SS
authors.lastname: Rahman
authors.forename: Steven
authors.initials: S
authors.lastname: Coulton
authors.forename: Hugh J
authors.initials: HJ
authors.lastname: Herdon
authors.forename: Graham F
authors.initials: GF
authors.lastname: Joiner
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
authors.forename: Roderick A
authors.initials: RA
authors.lastname: Porter
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D003198:Computer Simulation; D004353:Drug Evaluation, Preclinical; D050487:Glycine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors*; D006801:Humans; D007536:Isomerism; D008968:Molecular Conformation; D051381:Rats; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D050487:Glycine Plasma Membrane Transport Proteins; D013449:Sulfonamides