Journal of Medicinal Chemistry p. 538 - 544 (1983)
Update date:2022-09-26
Topics:
Bolhofer
Deana
Habecker
Hoffman
Gould
Pietruszkiewicz
Prugh
Torchiana
Cragoe Jr.
Hirschmann
A series of aminoalkyl-substituted pyridylureas has been prepared and evaluated as inhibitors of gastric acid secretion. N,N-Dimethyl-N'-[2-(diisopropylamino)ethyl-N'-(4,6-dimethyl-2-pyridyl)urea (8g) was the most potent example of the class. Comparison of this compound with cimetidine showed it to be equipotent in dogs stimulated with gastrin tetrapeptide but approximately half as potent in dogs stimulated with histamine. Inhibition of secretion does not appear to result from antagonism of the histamine H2 receptor, since the compounds show only weak inhibition of the H2 receptor in vitro.
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