Abstract
Screening of the Roche compound library led to the identification of the benzoylpiperazine 7 as a structurally novel GlyT1 inhibitor. The SAR which was developed in this series resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo efficacy after oral administration.
MeSH terms
-
Administration, Oral
-
Benzoates / chemistry*
-
Benzoates / pharmacology*
-
Brain / drug effects
-
Combinatorial Chemistry Techniques
-
Drug Design
-
Glycine Plasma Membrane Transport Proteins / antagonists & inhibitors*
-
Molecular Structure
-
Piperazines / chemistry*
-
Piperazines / pharmacology*
-
Structure-Activity Relationship
Substances
-
Benzoates
-
Glycine Plasma Membrane Transport Proteins
-
Piperazines