Novel 1-Hydroxyazole Bioisosteres of Glutamic Acid. Synthesis, Protolytic Properties, and Pharmacology

A number of 1-hydroxyazole derivatives were synthesized as bioisosteres of (S)-glutamic acid (Glu) and as analogues of the AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA, 3b). All compounds were subjected to in vitro pharmacological studies, including a s...

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Veröffentlicht in:	Journal of medicinal chemistry 2002-01, Vol.45 (1), p.19-31
Hauptverfasser:	Stensbøl, Tine B, Uhlmann, Peter, Morel, Sandrine, Eriksen, Birgitte L, Felding, Jakob, Kromann, Hasse, Hermit, Mette B, Greenwood, Jeremy R, Braüner-Osborne, Hans, Madsen, Ulf, Junager, Finn, Krogsgaard-Larsen, Povl, Begtrup, Mikael, Vedsø, Per
Format:	Artikel
Sprache:	eng
Schlagworte:	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - chemistry Animals Azoles - chemical synthesis Azoles - chemistry Azoles - pharmacology Biological and medical sciences Brain - drug effects Brain - metabolism Brain - physiology Carrier Proteins - metabolism CHO Cells COS Cells Cricetinae Electrophysiology Glutamatergic system (aspartate and other excitatory aminoacids) Glutamic Acid - chemistry Glutamine - metabolism In Vitro Techniques Male Medical sciences Models, Molecular Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Radioligand Assay Rats Rats, Sprague-Dawley Receptors, AMPA - agonists Receptors, AMPA - metabolism Structure-Activity Relationship Synaptosomes - metabolism
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