Title of article
Bridged bicyclic vasopressin receptor antagonists with V2-Selective or dual V1a/V2 activity
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
3081
To page
3084
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792604
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