Studies on 2(lH)-Quinolinone Derivatives as Gastric Antiulcer Active Agents. Synthesis and Antiulcer Activity of the Metabolites of 2-(4-Chlorobenzoylamino)-3-[2(lH)-quinolinon-4-yl] propionic Acid

Abstract

The metabolites of 2-(4-chlorobenzoylamino)-3-[2(lH)-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. © 1986, The Pharmaceutical Society of Japan. All rights reserved.