Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4 H)-yl)acetamide Vasopressin V 1b receptor antagonists

Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V 1b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4 H)-yl)acetamide have been identified with low nanomolar affinity for the V 1b receptor and good selectivity with respect to related r...

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Published inBioorganic & medicinal chemistry letters Vol. 21; no. 12; pp. 3813 - 3817
Main Authors Napier, Susan E., Letourneau, Jeffrey J., Ansari, Nasrin, Auld, Douglas S., Baker, James, Best, Stuart, Campbell-Wan, Leigh, Chan, Ray, Craighead, Mark, Desai, Hema, Ho, Koc-Kan, MacSweeney, Cliona, Milne, Rachel, Richard Morphy, J., Neagu, Irina, Ohlmeyer, Michael H.J., Pick, Jack, Presland, Jeremy, Riviello, Chris, Zanetakos, Heather A., Zhao, Jiuqiao, Webb, Maria L.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 15.06.2011
Subjects
Antagonist
HPA
V1b
HPA
V1b
Antagonist
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Summary:Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V 1b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4 H)-yl)acetamide 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 OT. Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.04.022