Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists

Min Amy Xiang; Robert H Chen; Keith T Demarest; Joseph Gunnet; Richard Look; William Hageman; William V Murray; Donald W Combs; Mona Patel

doi:10.1016/j.bmcl.2004.02.103

Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2987-9. doi: 10.1016/j.bmcl.2004.02.103.

Authors

Min Amy Xiang¹, Robert H Chen, Keith T Demarest, Joseph Gunnet, Richard Look, William Hageman, William V Murray, Donald W Combs, Mona Patel

Affiliation

¹ Endocrine Therapeutics and Metabolic Disorders, Johnson and Johnson Pharmaceutical Research and Development, L.L.C. 1000 Route 202, Bldg: PCC; Room: PC110, Raritan, NJ 08869-0602, USA.

PMID: 15125974
DOI: 10.1016/j.bmcl.2004.02.103

Abstract

A novel series of spirobenzazepines was synthesized and evaluated for V1a and V2 receptor antagonist activity. Compounds 8b, 8i, and 8k have shown selective V1a receptor antagonist activity. Compounds 8p and 8q were shown to be dual V1a/V2 receptor antagonists.

MeSH terms

Antidiuretic Hormone Receptor Antagonists*
Benzazepines / chemical synthesis
Benzazepines / pharmacology*
Cell Line
Cyclic AMP / analysis
Humans
Inhibitory Concentration 50
Ligands
Protein Binding
Spiro Compounds / chemical synthesis
Spiro Compounds / pharmacology*
Structure-Activity Relationship

Substances

Antidiuretic Hormone Receptor Antagonists
Benzazepines
Ligands
Spiro Compounds
Cyclic AMP