title: Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
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.
authors.affiliation: GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Pacofsky
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Stafford
authors.forename: Richard F
authors.initials: RF
authors.lastname: Cox
authors.forename: Jill R
authors.initials: JR
authors.lastname: Cowan
authors.forename: George F
authors.initials: GF
authors.lastname: Dorsey
authors.forename: Stephen S
authors.initials: SS
authors.lastname: Gonzales
authors.forename: Istvan
authors.initials: I
authors.lastname: Kaldor
authors.forename: George W
authors.initials: GW
authors.lastname: Koszalka
authors.forename: George G
authors.initials: GG
authors.lastname: Lovell
authors.forename: Maggie S
authors.initials: MS
authors.lastname: McIntyre
authors.forename: Jeffrey H
authors.initials: JH
authors.lastname: Tidwell
authors.forename: Dan
authors.initials: D
authors.lastname: Todd
authors.forename: Graham
authors.initials: G
authors.lastname: Whitesell
authors.forename: Robert P
authors.initials: RP
authors.lastname: Wiard
authors.forename: Paul L
authors.initials: PL
authors.lastname: Feldman
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D015195:Drug Design; D058785:GABA-A Receptor Agonists; D007202:Indicators and Reagents; D008968:Molecular Conformation; D004856:Postural Balance / Q000187:drug effects; D051381:Rats; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D058785:GABA-A Receptor Agonists; D007202:Indicators and Reagents; D001569:Benzodiazepines