Stereoselective synthesis and preliminary evaluation of new D-3-heteroarylcarbonylalanines as ligands of the NMDA receptor

Autor:	Renata Fittipaldi Pessoa, Newton G. Castro, Paulo R. R. Costa, D. L. Mendonça-Silva, Rodrigo R.B. Caruso, Paulo G. de Lima, François Noël, Simone O. Alves, Ricardo José Nunes
Rok vydání:	2004
Předmět:	Stereochemistry Clinical Biochemistry Allosteric regulation Drug Evaluation Preclinical Pharmaceutical Science Thiophenes Ligands Biochemistry Chemical synthesis Receptors N-Methyl-D-Aspartate chemistry.chemical_compound Pyridine Drug Discovery Thiophene medicine Animals Rats Wistar Molecular Biology Glycine receptor Cerebral Cortex Alanine Chemistry Organic Chemistry Glutamate receptor Biological activity Stereoisomerism General Medicine Rats medicine.anatomical_structure nervous system Glycine Molecular Medicine NMDA receptor Stereoselectivity Neuron Dizocilpine Maleate Derivative (chemistry) Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 14(17)
ISSN:	0960-894X
Popis:	New N-heteroarylcarbonylalanines of the D-series were stereoselectively prepared from enoates derived from D-mannitol. These compounds were active in binding and functional assays of the NMDA sub-type of glutamate receptors. A pyridine derivative inhibited MK801 binding, protected neurons from excitotoxic damage and blocked NMDA-induced currents in neurons. A thiophene derivative positively modulated the NMDA receptor, possibly through the allosteric glycine site.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::380f35af75d618115f979a1801e2f895 https://pubmed.ncbi.nlm.nih.gov/15357961 Zobrazit plný text záznamu Full Text from ScienceDirect