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Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
Pacofsky, Gregory J; Stafford, Jeffrey A; Cox, Richard F; Cowan, Jill R; Dorsey, George F; Gonzales, Stephen S; Kaldor, Istvan; Koszalka, George W; Lovell, George G; McIntyre, Maggie S; Tidwell, Jeffrey H; Todd, Dan; Whitesell, Graham; Wiard, Robert P; Feldman, Paul L.
Bioorg Med Chem Lett ; 12(21): 3219-22, 2002 Nov 04.
Article in English | MEDLINE | ID: mdl-12372538

ABSTRACT

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.


Subject(s)
Benzodiazepines/chemical synthesis , Benzodiazepines/pharmacology , GABA-A Receptor Agonists , Animals , Benzodiazepines/pharmacokinetics , Drug Design , Indicators and Reagents , Molecular Conformation , Postural Balance/drug effects , Rats , Solubility , Structure-Activity Relationship
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