2. Academic Validation
  3. Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists

  • Bioorg Med Chem Lett. 2003 Feb 24;13(4):753-6. doi: 10.1016/s0960-894x(02)01059-4.
Jay M Matthews 1,  Michael N Greco,  Leonard R Hecker,  William J Hoekstra,  Patricia Andrade-Gordon,  Lawrence de Garavilla,  Keith T Demarest,  Eric Ericson,  Joseph W Gunnet,  William Hageman,  Richard Look,  John B Moore,  Bruce E Maryanoff
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477-0776, USA. jmatthew@prius.jnj.com
PMID: 12639574 DOI: 10.1016/s0960-894x(02)01059-4
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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