Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide Vasopressin V₁b receptor antagonists
2011
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.
Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V₁b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V₁b receptor and good selectivity with respect to related receptors V₁ₐ, V₂ and OT. Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.
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