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ID: ALA1134932
Journal: Bioorg Med Chem Lett
Title: Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.
Authors: Dyatkin AB, Hoekstra WJ, Hlasta DJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Gunnet JW, Hageman W, Look R, Maryanoff BE.
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 (R(1)-R(3)) in general formula 3, and the configuration of the stereocenter, resulted in potent V(2)-selective (e.g., 5) and balanced dual V(1a)/V(2) (e.g., 10) compounds. Data from receptor binding, cell-based functional, and in vivo assays are presented [corrected]
CiteXplore: 12372506