title: Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
abstract: Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and OT. Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.
authors: Department of Chemistry, MSD, Newhouse, Lanarkshire, UK. susan.napier@spcorp.com
authors: Susan E
authors: SE
authors: Napier
authors: Jeffrey J
authors: JJ
authors: Letourneau
authors: Nasrin
authors: N
authors: Ansari
authors: Douglas S
authors: DS
authors: Auld
authors: James
authors: J
authors: Baker
authors: Stuart
authors: S
authors: Best
authors: Leigh
authors: L
authors: Campbell-Wan
authors: Ray
authors: R
authors: Chan
authors: Mark
authors: M
authors: Craighead
authors: Hema
authors: H
authors: Desai
authors: Koc-Kan
authors: KK
authors: Ho
authors: Cliona
authors: C
authors: MacSweeney
authors: Rachel
authors: R
authors: Milne
authors: J
authors: J
authors: Richard Morphy
authors: Irina
authors: I
authors: Neagu
authors: Michael H J
authors: MH
authors: Ohlmeyer
authors: Jack
authors: J
authors: Pick
authors: Jeremy
authors: J
authors: Presland
authors: Chris
authors: C
authors: Riviello
authors: Heather A
authors: HA
authors: Zanetakos
authors: Jiuqiao
authors: J
authors: Zhao
authors: Maria L
authors: ML
authors: Webb