Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists

…, JR Cowan, GF Dorsey, SS Gonzales, I Kaldor…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 21 p. 3219 - 3222

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Citation Number: 13

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.