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Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists
Gregory J Pacofsky1, Jeffrey A Stafford, Richard F Cox
1GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
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.