| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370846 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Susan E. Napier, Jeffrey J. Letourneau, Nasrin Ansari, Douglas S. Auld, James Baker, Stuart Best, Leigh Campbell-Wan, Ray Chan, Mark Craighead, Hema Desai, Koc-Kan Ho, Cliona MacSweeney, Rachel Milne, J. Richard Morphy, Irina Neagu,