Author/Authors :
Alexey B. Dyatkin، نويسنده , , William J. Hoekstra، نويسنده , , Dennis J. Hlasta، نويسنده , , Patricia Andrade-Gordon، نويسنده , , Lawrence de Garavilla، نويسنده , , Keith T. Demarest، نويسنده , , Joseph W. Gunnet، نويسنده , , William Hageman، نويسنده , , Richard Look، نويسنده , , Bruce E. Maryanoff، نويسنده ,
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 (e.g., 4) and balanced dual V1a/V2 (e.g., 10) compounds. Data from receptor binding, cell-based functional, and in vivo assays are presented.
