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Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists. 2002
Jeffrey A Stafford, and
Gregory J Pacofsky, and
Richard F Cox, and
Jill R Cowan, and
George F Dorsey, and
Stephen S Gonzales, and
David K Jung, and
George W Koszalka, and
Maggie S McIntyre, and
Jeffrey H Tidwell, and
Robert P Wiard, and
Paul L Feldman
GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
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.
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