Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
Bioorg Med Chem Lett
; 18(20): 5533-6, 2008 Oct 15.
Article
in En
| MEDLINE
| ID: mdl-18805008
ABSTRACT
Several novel classes of potent and small amide-type inhibitors of glycine transport (GlyT1) were developed through sequential simplification of a benzodiazepinone-lead structure identified from a high-throughput screening. The most potent compounds of these structurally simple classes show low nanomolar inhibition at the GlyT1 target.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Chemistry, Pharmaceutical
/
Glycine Plasma Membrane Transport Proteins
/
Amides
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country:
Switzerland