1,2,3-Triazolyl amino acids as AMPA receptor ligands

The central nervous system glutamate receptors are an important target for drug discovery. Herein we report initial investigations into the synthesis and glutamate receptor activity of 1,2,3-triazolyl amino acids. Two compounds were found to be selective AMPA receptor ligands, which warrant further...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (24), p.7512-7515
Hauptverfasser:	Stanley, N.J., Pedersen, D. Sejer, Nielsen, B., Kvist, T., Mathiesen, J.M., Bräuner-Osborne, H., Taylor, D.K., Abell, A.D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acids - chemical synthesis Amino Acids - chemistry Amino Acids - pharmacology Binding Sites Biological and medical sciences Catalysis Computer Simulation Copper - chemistry Glutamate receptor Glutamatergic system (aspartate and other excitatory aminoacids) Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptors, AMPA - antagonists & inhibitors Receptors, AMPA - metabolism Ruthenium - chemistry Synthesis Triazole Triazoles - chemistry
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Zusammenfassung:	The central nervous system glutamate receptors are an important target for drug discovery. Herein we report initial investigations into the synthesis and glutamate receptor activity of 1,2,3-triazolyl amino acids. Two compounds were found to be selective AMPA receptor ligands, which warrant further investigation.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.09.139