Sarcosine based indandione hGlyT1 inhibitors

Christopher G Thomson; Karen Duncan; Stephen R Fletcher; Ian T Huscroft; Gopalan Pillai; Piotr Raubo; Alison J Smith; Darren Stead

doi:10.1016/j.bmcl.2005.11.041

Sarcosine based indandione hGlyT1 inhibitors

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1388-91. doi: 10.1016/j.bmcl.2005.11.041.

Authors

Christopher G Thomson¹, Karen Duncan, Stephen R Fletcher, Ian T Huscroft, Gopalan Pillai, Piotr Raubo, Alison J Smith, Darren Stead

Affiliation

¹ 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

PMID: 16321523
DOI: 10.1016/j.bmcl.2005.11.041

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.

MeSH terms

Glycine Plasma Membrane Transport Proteins / antagonists & inhibitors*
Glycine Plasma Membrane Transport Proteins / metabolism
Humans
Inhibitory Concentration 50
Molecular Structure
Sarcosine / chemical synthesis
Sarcosine / chemistry*
Sarcosine / pharmacology*
Sensitivity and Specificity
Structure-Activity Relationship
Substrate Specificity

Substances

Glycine Plasma Membrane Transport Proteins
SLC6A9 protein, human
Sarcosine