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A series of (3-substituted phenyl)urea analogues of the potent gastrin/cholecystokinin (CCK)-B receptor antagonist YM022 has been prepared. Structure-activity relationship studies of this series suggested that a number of analogues retained good in vitro potency for gastrin/CCK-B receptor. In particular, the (3-amino substituted phenyl)urea derivatives (10-12) were more potent inhibitors of pentagastrin-induced gastric acid secretion in rats than YM022 on intraduodenal (i.d.) administration.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Biological Activity of Analogues of YM022. Novel (3-Amino Substituted Phenyl)urea Derivatives of 1,4-Benzodiazepin-2-one as Gastrin/Cholecystokinin-B Receptor Antagonists.