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Bioorg Med Chem Lett. 2011 Mar 15;21(6):1871-5. doi: 10.1016/j.bmcl.2010.12.081. Epub 2010 Dec 21.

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Author information

1
Department of Chemistry, MSD, Newhouse, Lanarkshire, UK. susannapier67@googlemail.com

Abstract

Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and oxytocin (OT). Optimised compound 12j demonstrates a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.

PMID:
21353540
DOI:
10.1016/j.bmcl.2010.12.081
[Indexed for MEDLINE]

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