Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists

Autor:	Dan Todd, George W. Koszalka, Richard F. Cox, Jeffrey H. Tidwell, Graham Whitesell, Jeffrey A. Stafford, Robert P. Wiard, Gregory J. Pacofsky, Paul L. Feldman, George G. Lovell, Stephen S. Gonzales, Jill R. Cowan, Maggie S. McIntyre, Istvan Kaldor, George F. Dorsey
Rok vydání:	2002
Předmět:	Agonist Annulation Stereochemistry medicine.drug_class Clinical Biochemistry Molecular Conformation Pharmaceutical Science Biochemistry Chemical synthesis Benzodiazepines Structure-Activity Relationship Drug Discovery Aqueous solubility medicine Structure–activity relationship Animals GABA-A Receptor Agonists Receptor Molecular Biology Postural Balance Benzodiazepine Chemistry Organic Chemistry Rats Solubility Drug Design Molecular Medicine Indicators and Reagents
Zdroj:	Bioorganicmedicinal chemistry letters. 12(21)
ISSN:	0960-894X
Popis:	The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the C5-haloaryl ring, and annulation of heterocycles are presented. These analogues retain BZD receptor potency and full agonism profiles.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a244e355ade8e1e21ea366fa371db62 https://pubmed.ncbi.nlm.nih.gov/12372538 Zobrazit plný text záznamu Full Text from ScienceDirect