SYNTHESIS AND ANTIULCER ACTIVITY OF 3,4-DIHYDRO-HAINANENSINE ANALOGS

In order to search for new compounds with new mode of action, high antiulcer activity and lower toxicity, 26(13 pairs of diastereoisomer A and B) 3,4-dihydro-hananensine analogs were synthesized. All compounds were tested in M₁ receptor combined assay and gastric ulcer induced by cold-immersion stress in rats. Most compounds showed antiulcer activity, among them IX₃A, IX₇A, IX₈A, IX₁₂A, IX₁₂B and IX₁₃A exhibited more potent antiulcer activity than the control compound cimetidine. Meanwhile, the relationship between their structures and activity was discussed. 