Bioorganic and Medicinal Chemistry Letters p. 3219 - 3222 (2002)
Update date:2022-08-03
Topics: Chemical Structure Pharmacokinetics Clinical Applications Physical Properties
Pacofsky, Gregory J.
Stafford, Jeffrey A.
Cox, Richard F.
Cowan, Jill R.
Dorsey Jr., George F.
Gonzales, Stephen S.
Kaldor, Istvan
Koszalka, George W.
Lovell, George G.
McIntyre, Maggie S.
Tidwell, Jeffrey H.
Todd, Dan
Whitesell, Graham
Wiard, Robert P.
Feldman, Paul L.
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.
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