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

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

oai:eprints.gla.ac.uk:129017

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

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

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oai:eprints.gla.ac.uk:129017

Last time updated on 12/10/2016

This paper was published in Enlighten.

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