Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

A novel series of 1-alkylcarbonylmethyl analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared. A number of analogues retained good affinity for the gastrin/CCK-B receptor and one compound ( 6d) showed improved binding and enhanced selectivity for this receptor over CCK-A...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-01, Vol.6 (1), p.51-54
Main Authors: Semple, Graeme, Ryder, Hamish, Kendrick, David A., Szelke, Michael, Ohta, Mitsuaki, Satoh, Masato, Nishida, Akito, Akuzawa, Shinobu, Miyata, Keiji
Format: Article
Language:English
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Summary:A novel series of 1-alkylcarbonylmethyl analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared. A number of analogues retained good affinity for the gastrin/CCK-B receptor and one compound ( 6d) showed improved binding and enhanced selectivity for this receptor over CCK-A. A second compound ( 6j) gave improved in vivo inhibition of gastric acid secretion in rats. Both analogues were shown to have significantly better activity in the same model following i.d. dosing than either YM022 or L-365,260. A novel series of 1-alkylcarbonylmethyl analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared. Several analogues retained good affinity for the gastrin/CCK-B receptor. Compounds 6d and 6j were superior to both YM022 or L-365,260 in in vivo models of acid secretion.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00556-9