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ID: ALA1133037

Journal: Bioorg Med Chem Lett

Title: The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.

Authors: Ashwell MA, Bagli JF, Caggiano TJ, Chan PS, Molinari AJ, Palka C, Park CH, Rogers JF, Sherman M, Trybulski EJ, Williams DK.

Abstract: Ionizable groups were introduced onto the 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine scaffold of the vasopressin V2-antagonist WAY-VPA-985 in the search for molecules optimized for parenteral formulation. The synthesis and structure activity relationships (SAR) are presented together with solubility data in a model parenteral system. The amine, WAY-140288 (4f), was chosen for further development. p6

CiteXplore: 10782686

DOI: 10.1016/s0960-894x(00)00095-0