Ontology highlight
ABSTRACT:
SUBMITTER: Clausen RP
PROVIDER: S-EPMC4850074 | biostudies-literature | 2008 Jul
REPOSITORIES: biostudies-literature
Clausen Rasmus P RP Christensen Caspar C Hansen Kasper B KB Greenwood Jeremy R JR Jørgensen Lars L Micale Nicola N Madsen Jens Christian JC Nielsen Birgitte B Egebjerg Jan J Bräuner-Osborne Hans H Traynelis Stephen F SF Kristensen Jesper L JL
Journal of medicinal chemistry 20080625 14
A series of analogues based on N-hydroxypyrazole as a bioisostere for the distal carboxylate group of aspartate have been designed, synthesized, and pharmacologically characterized. Affinity studies on the major glutamate receptor subgroups show that these 4-substituted N-hydroxypyrazol-5-yl glycine (NHP5G) derivatives are selectively recognized by N-methyl- d-aspartic acid (NMDA) receptors and that the ( R)-enantiomers are preferred. Moreover, several of the compounds are able to discriminate b ...[more]