Paper
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
Published Dec 1, 1987 · A. A. Santilli, A. Scotese, R. Bauer
Journal of medicinal chemistry
50
Citations
0
Influential Citations
Abstract
The syntheses of 2-oxo-1,8-naphthyridine-3-carboxylic acid derivatives having potent gastric antisecretory properties in the pyloric-ligated (Shay) rat model are described. Two of the more potent compounds tested that were selected for more detailed dose-response evaluation were 4-amino-1-ethyl-1,2-dihydro-2-oxonaphthyridine-3-carboxylic acid ethyl ester (35) and 1-ethyl-1,2-dihydro-7-methyl-4-(4-methyl-1-piperazinyl)-2- oxo-1,8-naphthyridine-3-carboxylic acid ethyl ester (77). These compounds lowered total acid output in the rat in a dose-related fashion. Both compounds were more potent than cimetidine when tested in the rat. Both 35 and 77 showed inhibitory activity in food-stimulated acid secretion in the Pavlov-pouch, conscious dog. The mechanism of action for this series is not known. Details of structure-activity relationships are described.
Non-RCT
Animal Study2-oxo-1,8-naphthyridine-3-carboxylic acid derivatives show potent gastric antisecretory properties, with compounds 35 and 77 being more potent than cimetidine in lowering total acid output in the rat and food-stimulated acid secret
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