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

Napier, S. E. et al. (2011) Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 21(6), pp. 1871-1875. (doi:10.1016/j.bmcl.2010.12.081)

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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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Thomson, Dr Fiona
Authors: Napier, S. E., Letourneau, J. J., Ansari, N., Auld, D. S., Baker, J., Best, S., Campbell-Wan, L., Chan, J.-H., Craighead, M., Desai, H., Goan, K. A., Ho, K.-K., Hulskotte, E. G.J., MacSweeney, C. P., Milne, R., Morphy, J. R., Neagu, I., Ohlmeyer, M. H.J., Peeters, A. W.M.M., Presland, J., Riviello, C., Ruigt, G. S.F., Thomson, F. J., Zanetakos, H. A., Zhao, J., and Webb, M. L.
College/School:College of Medical Veterinary and Life Sciences > Institute of Cancer Sciences
Journal Name:Bioorganic and Medicinal Chemistry Letters
Publisher:Elsevier
ISSN:0960-894X
Published Online:21 December 2010

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