Bioorganic and Medicinal Chemistry Letters p. 3215 - 3218 (2002)
Update date:2022-09-26
Stafford,, Jeffrey A.
Pacofsky,, Gregory J.
Cox, Richard F.
Cowan, Jill R.
Dorsey Jr., George F.
Gonzales, Stephen S.
Jung, David K.
Koszalka, George W.
McIntyre, Maggie S.
Tidwell, Jeffrey H.
Wiard, Robert P.
Feldman, Paul L.
The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are 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.
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Doi:10.1039/JR9570003708
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