Bioorganic and Medicinal Chemistry Letters p. 51 - 54 (1996)
Update date:2022-08-03
Topics:
Semple, Graeme
Ryder, Hamish
Kendrick, David A.
Szelke, Michael
Ohta, Mitsuaki
Satoh, Masato
Nishida, Akito
Akuzawa, Shinobu
Miyata, Keiji
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.
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