Sarcosine based indandione hGlyT1 inhibitors.
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.
Thomson
Christopher G
CG
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
Duncan
Karen
K
Fletcher
Stephen R
SR
Huscroft
Ian T
IT
Pillai
Gopalan
G
Raubo
Piotr
P
Smith
Alison J
AJ
Stead
Darren
D
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
D050487:Glycine Plasma Membrane Transport Proteins; C493268:SLC6A9 protein, human; D012521:Sarcosine