Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands

A Cordi; J M Lacoste; V Audinot; M Millan

doi:10.1016/s0960-894x(99)00194-8

Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands

Bioorg Med Chem Lett. 1999 May 17;9(10):1409-14. doi: 10.1016/s0960-894x(99)00194-8.

Authors

A Cordi¹, J M Lacoste, V Audinot, M Millan

Affiliation

¹ Institut de Recherches Servier, Suresnes, France. cordi@netgrs.com

PMID: 10360746
DOI: 10.1016/s0960-894x(99)00194-8

Abstract

The in vitro activities of 3-hydroxy-imidazolidin-4-one derivatives demonstrated very restricted structure-activity relationships at the strychnine-insensitive glycine site of the NMDA receptor. The most active compound (3a) was completely unsubstituted and exhibited affinity and efficacy similar to that of D-cycloserine, the prototypical partial agonist at this site.

MeSH terms

Drug Design*
Glycine / metabolism*
Imidazoles / chemical synthesis
Imidazoles / chemistry*
Imidazoles / pharmacology*
Ligands
Receptors, N-Methyl-D-Aspartate / chemistry
Receptors, N-Methyl-D-Aspartate / metabolism*
Structure-Activity Relationship
Strychnine / pharmacology*

Substances

3-hydroxyimidazolidin-4-one
Imidazoles
Ligands
Receptors, N-Methyl-D-Aspartate
Strychnine
Glycine