Abstract
Anti-ulcer activity of newly synthesized acylquinoline derivatives was investigated. For thein vitro screening, the effects of the compounds on gastric H+/K+ ATPase isolated from hog and rabbit were examined. Among them, AU-090, AU-091, AU-254, AU-413 and AU-466 exhibited goodin vitro activity on both enzymes. To correlate thein vitro activity within vivo action, the effects of the compounds on the basal gastric acid secretion were studied. Some derivatives showed considerable anti-secretory activities, and AU-413 was selected for further studies. AU-413 protected gastric damage induced by either ethanol or NaOH dose dependently when given orally. ED50 values of 12 mg/kg,p.o. (ethanol) and 41 mg/kg,p.o. (NaOH) were obtained. In addition, histamine-stimulated gastric secretion was reduced upon AU-413 administration. Taken together, newly synthesized acylquinoline derivatives, especially AU-413, is worthy of further investigation to be developed as an anti-ulcer agent.
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Cheon, H.G., Kim, H.J., Mo, H.K. et al. Anti-ulcer activity of newly synthesized acylquinoline derivatives. Arch Pharm Res 22, 137–142 (1999). https://doi.org/10.1007/BF02976537
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DOI: https://doi.org/10.1007/BF02976537