Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates

Autor:	Dennis J. Hlasta, Richard Look, Eric Ericson, Joseph W. Gunnet, Brenda L. Poulter, Leonard R. Hecker, Charles H. Reynolds, Bruce E. Maryanoff, Lawrence de Garavilla, Matthews Jay M, John B. Moore, Keith T. Demarest, William Hageman, William J. Hoekstra, Patricia Andrade-Gordon, Alexey B. Dyatkin
Rok vydání:	2004
Předmět:	Vasopressin Arginine Clinical Biochemistry Thiazines Administration Oral Pharmaceutical Science Pharmacology Biochemistry Rats Sprague-Dawley Benzodiazepines Structure-Activity Relationship Aquaretic Arginine vasopressin receptor 2 Oxazines Drug Discovery Animals Humans Diuretics Receptor Molecular Biology Vasopressin receptor Arginine vasopressin receptor 1B chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Rats Molecular Medicine Antidiuretic Hormone Receptor Antagonists Protein Binding Tricyclic
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 14:2747-2752
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2004.03.083
Popis:	Vasopressin receptor antagonists can elicit ion-sparing diuretic effects (i.e., aquaresis) in vivo by blunting the action of the circulating hypophyseal hormone arginine vasopressin. We have identified two new series of basic tricyclic benzodiazepines, represented by general structure 1, which contain compounds that bind with high affinity to human V2 receptors. For example, (S)-(+)-8 and 5 are potent and selective V2 receptor antagonists with pronounced aquaretic activity in rats on oral administration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b7266f2003e8bbde0bb5f0561f6f867 https://doi.org/10.1016/j.bmcl.2004.03.083 Zobrazit plný text záznamu Full Text from ScienceDirect