Identification and Structure–Activity Studies of Novel Ultrashort-Acting Benzodiazepine Receptor Agonists

The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxyl...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-11, Vol.12 (21), p.3215-3218
Hauptverfasser:	Stafford, Jeffrey A., Pacofsky, Gregory J., Cox, Richard F., Cowan, Jill R., Dorsey, George F., Gonzales, Stephen S., Jung, David K., Koszalka, George W., McIntyre, Maggie S., Tidwell, Jeffrey H., Wiard, Robert P., Feldman, Paul L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzodiazepines - chemical synthesis Benzodiazepines - pharmacokinetics Benzodiazepines - pharmacology Biological and medical sciences Chromatography, High Pressure Liquid GABA-A Receptor Agonists Gabaergic and benzodiazepinic system Humans Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Postural Balance - drug effects Rats Receptors, GABA-A - metabolism Structure-Activity Relationship
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Zusammenfassung:	The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles.©2000 Elsevier Science Ltd. All rights reserved.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00512-7