Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 53 (12), 4603-14

Selective GlyT1 Inhibitors: Discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine to Treat Schizophrenia

Affiliations

Selective GlyT1 Inhibitors: Discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine to Treat Schizophrenia

Emmanuel Pinard et al. J Med Chem.

Abstract

The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve hERG channel selectivity and brain penetration. This effort culminated in the discovery of compound 10a (RG1678), the first potent and selective GlyT1 inhibitor to have a beneficial effect in schizophrenic patients in a phase II clinical trial.

Similar articles

See all similar articles

Cited by 31 PubMed Central articles

See all "Cited by" articles

MeSH terms

Substances

LinkOut - more resources

Feedback