Studies on 2 (1H) -Quinolinone Derivatives as Gastric Antiulcer Active Agents. Synthesis and Antiulcer Activities of Optically Active α-Amino Acid Derivatives of 2 (1H) -Quinolinone and Oxindole

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In order to study the relationship of structure to antiulcer activity, optical active α-amino acid derivatives of 2 (1H) -quinolinone and oxindole were synthesized and tested for antiulcer activity against acetic acid-induced gastric ulcer in rats. The enantiomers of 2 (1H) -quinolinone derivatives were obtained by optical resolution with (-) -brucine. The oxindole derivatives having different absolute configurations at the α-amino acid moiety were synthesized by oxidation of N- (4- chlorobenzoyl) -L- or -D-tryptophan. The antiulcer activity did not seem to be influenced by the α-amino acid chirality.