Journal of medicinal chemistry · 1983
Gastric antisecretory 9H-xanthen-9-amines.
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Bender P E, Perchonock C D, Groves W G, Smith R C, Stringer O D, Sneed R, Schlosser J H, Hostelley L S, Hwang B Y, Eby R Z, Konicki G, Lavanchy P G, Wilson J W, Loev B
Аннотация
A series of 9H-xanthen-9-amines possessing a wide variety of nitrogen substituents at C-9 was prepared for evaluation of gastric antisecretory activity. These substituents included the acetamidine, imidate, pyrimidine, thiazoline, quinuclidine, 2-hydrazinopyridine, aminopiperidine, aminoalkylimidazole, and aminoalkylpyridine moieties. The majority of compounds in this series inhibited gastric acid secretion when tested orally in the pylorus-ligated rat. Potency was increased by intraduodenal administration and diminished by incubation with gastric juice, suggesting partial degradation of the compounds in the gastric environment. A representative example, 3-(9H-xanthen-9-ylamino)-1-ethylpiperidine, exhibited similar activity in dogs, although no free compound could be detected in the blood. It is therefore hypothesized that this compound is either rapidly bound to tissue and/or metabolized to an active species.