Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.
Bioorg Med Chem Lett
; 20(23): 6960-5, 2010 Dec 01.
Article
in En
| MEDLINE
| ID: mdl-20974532
ABSTRACT
Benzoylisoindolines were discovered as a novel structural class of GlyT1 inhibitors. SAR studies and subsequent lead optimization efforts focused primarily on addressing hERG liability and on improving in vivo efficacy resulted in the identification of potent GlyT1 inhibitors displaying excellent selectivity and in vivo PD and PK profiles.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Glycine Plasma Membrane Transport Proteins
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Document type:
Article
Affiliation country:
Switzerland