Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists
Bioorganic & Medicinal Chemistry LettersPublished 1 February 2003Open access
Jay M. Matthews, Michael N. Greco, Leonard R. Hecker, William J. Hoekstra, Patricia Andrade‐Gordon, Lawrence de Garavilla
Citations36
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TL;DR
A series of novel 3,4,5,6-tetrahydro-1H-azepino[4,3,2-cd]indoles was synthesized and tested for vasopressin receptor antagonist activity and identified compounds with high affinity for the human V2 receptor and good selectivity over the humanV1a receptor.
Abstract
A series of novel 3,4,5,6-tetrahydro-1H-azepino[4,3,2-cd]indoles was synthesized and tested for vasopressin receptor antagonist activity. We identified compounds with high affinity for the human V2 receptor and good selectivity over the human V1a receptor. Compound 6c bound to V2 receptors with an IC(50) value of 20 nM, had >100-fold selectivity over V1a receptors, and inhibited cAMP formation in a cellular V2 functional assay with an IC(50) value of 70 nM.
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