Furo[3,2-h]quinoline derivatives were synthesized as a gastric $H^+$/$K^+$-ATPase inhibitors. The oxycyclization of 7 and 8-positions in quinoline potentiated the inhibitory activity, while no significant changes in biological activity were observed by the variation of substituents in furan ring. The several furo[3,2-h]quinoline derivatives were worthy of in vivo investigation for their anti-secretory and anti-ulcer activity.