Studies on 2(1H)-quinolinone derivatives as gastric antiulcer active agents. Synthesis and antiulcer activity of the metabolites of 2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinon-4-yl)propionic acid.

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Abstract
The metabolites of 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic acid (OPC-12759) (1), which has a potent antiulcer activity towards acetic acid-induced gastric ulcer, were synthesized to confirm their structures and to examine their antiulcer activity. The structures of the major metabolites (2-4) in the rat were identified by means of comparisons with the synthetic compounds. The antiulcer activity of the metabolites (2-4) was found to be lower than that of 1.

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