1314039-72-9Relevant academic research and scientific papers
Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo- 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, Ray,Craighead, Mark,Desai, Hema,Ho, Koc-Kan,MacSweeney, Cliona,Milne, Rachel,Richard Morphy,Neagu, Irina,Ohlmeyer, Michael H.J.,Pick, Jack,Presland, Jeremy,Riviello, Chris,Zanetakos, Heather A.,Zhao, Jiuqiao,Webb, Maria L.
, p. 3813 - 3817 (2011/08/02)
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.
