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

By Susan E. Napier, Jeffrey J. Letourneau, Nasrin Ansari, Douglas S. Auld, James Baker, Stuart Best, Leigh Campbell-Wan, Jui-Hsiang Chan, Mark Craighead, Hema Desai, Katharine A. Goan, Koc-Kan Ho, Ellen G.J. Hulskotte, Cliona P. MacSweeney, Rachel Milne, J. Richard Morphy, Irina Neagu, Michael H.J. Ohlmeyer, Ard W.M.M. Peeters, Jeremy Presland, Chris Riviello, Ge S.F. Ruigt, Fiona J. Thomson, Heather A. Zanetakos, Jiuqiao Zhao and Maria L. Webb

Abstract

Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V1b (V3) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V1b receptor and good selectivity with respect to related receptors V1a, V2 and oxytocin (OT). Optimised compound 12j demonstrates a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction

Publisher: Elsevier
Year: 2011
OAI identifier: oai:eprints.gla.ac.uk:129017
Provided by: Enlighten
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