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Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists
Jeffrey A Stafford1, Gregory J Pacofsky, Richard F Cox
1GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
Abstract:
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.