Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists

Autor:	David Kendall Jung, Jeffrey A. Stafford, Maggie S. McIntyre, George F. Dorsey, Robert P. Wiard, Gregory J. Pacofsky, Jeffrey H. Tidwell, Paul L. Feldman, Jill R. Cowan, George W. Koszalka, Richard F. Cox, Stephen S. Gonzales
Rok vydání:	2002
Předmět:	Agonist Stereochemistry medicine.drug_class Metabolite Carboxylic acid Clinical Biochemistry Pharmaceutical Science Biochemistry chemistry.chemical_compound Benzodiazepines Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Animals Humans GABA-A Receptor Agonists Molecular Biology Postural Balance Chromatography High Pressure Liquid chemistry.chemical_classification Benzodiazepine Organic Chemistry Glutamic acid Receptors GABA-A Amino acid Rats chemistry Propionate Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 12(21)
ISSN:	0960-894X
Popis:	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. Copyright2000 Elsevier Science Ltd.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99d047ea53933821c04309d99379650d https://pubmed.ncbi.nlm.nih.gov/12372537 Zobrazit plný text záznamu Full Text from ScienceDirect