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

DOI: 10.1248/cpb.44.1412

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1412 - 1414 (1996)

Update date:2022-09-26

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Authors:

Satoh, Masato

Okamoto, Yoshinori

Koshio, Hiroyuki

Ohta, Mitsuaki

Nishida, Akito

Akuzawa, Shinobu

Miyata, Keiji

Mase, Toshiyasu

Semple, Graeme

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Article abstract of DOI:10.1248/cpb.44.1412

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.

Full text of DOI:10.1248/cpb.44.1412

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