title: Sarcosine based indandione hGlyT1 inhibitors.
abstract: A series of sarcosine based indandione hGlyT1 inhibitors has been developed. Optimization of substitution around the indandione and sarcosine moieties has led to highly potent inhibitors at hGlyT1, which show selectivity over a number of other receptors.
authors.affiliation: Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. christopher_thompson@merck.com
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Thomson
authors.forename: Karen
authors.initials: K
authors.lastname: Duncan
authors.forename: Stephen R
authors.initials: SR
authors.lastname: Fletcher
authors.forename: Ian T
authors.initials: IT
authors.lastname: Huscroft
authors.forename: Gopalan
authors.initials: G
authors.lastname: Pillai
authors.forename: Piotr
authors.initials: P
authors.lastname: Raubo
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Smith
authors.forename: Darren
authors.initials: D
authors.lastname: Stead
mesh_terms: D050487:Glycine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D012521:Sarcosine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D050487:Glycine Plasma Membrane Transport Proteins; C493268:SLC6A9 protein, human; D012521:Sarcosine