Bridged bicyclic vasopressin receptor antagonists with V 2-Selective or dual V 1a/V 2 activity

…, DJ Hlasta, P Andrade-Gordon, L de Garavilla…

Index: Dyatkin, Alexey B.; Hoekstra, William J.; Hlasta, Dennis J.; Andrade-Gordon, Patricia; De Garavilla, Lawrence; Demarest, Keith T.; Gunnet, Joseph W.; Hageman, William; Look, Richard; Maryanoff, Bruce E. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 21 p. 3081 - 3084

Full Text: HTML

Citation Number: 17

Abstract

The synthesis and biological testing of a novel series of nonpeptide vasopressin receptor antagonists, containing a bridged bicyclic nucleus, are reported. Variation of substituents (R1–R3) in general formula 3, and the configuration of the stereocenter, resulted in potent V2-selective (eg, 4) and balanced dual V1a/V2 (eg, 10) compounds. Data from receptor binding, cell-based functional, and in vivo assays are presented.