Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists |
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| Authors: | Matthews Jay M Greco Michael N Hecker Leonard R Hoekstra William J Andrade-Gordon Patricia de Garavilla Lawrence Demarest Keith T Ericson Eric Gunnet Joseph W Hageman William Look Richard Moore John B Maryanoff Bruce E |
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| Institution: | Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477-0776, USA. jmatthew@prius.jnj.com |
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| Abstract: | A series of novel 3,4,5,6-tetrahydro-1H-azepino4,3,2-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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