3,4-二氢-海南新碱类似物的合成及抗溃疡作用

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

为考察３，４二氢海南新碱类似物Ｃ１取代基对化合物抗溃疡活性的影响，设计并合成了１３对共２６个新的３，４二氢海南新碱类似物，Ａ，Ｂ互为非对映异构体，大部分化合物在大鼠冷应激溃疡模型中有一定的抗溃疡活性，其中ＩＸ３Ａ，ＩＸ７Ａ，ＩＸ８Ａ，ＩＸ１２Ａ，ＩＸ１２Ｂ，ＩＸ１３Ａ６个化合物表现较强活性，超过西咪替丁。

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 M1 receptor combined assay and gastric ulcer induced by coldimmersion stress in rats. Most compounds showed antiulcer activity, among them IX3A, IX7A, IX8A, IX12A, IX12B and IX13A exhibited more potent antiulcer activity than the control compound cimetidine. Meanwhile, the relationship between their structures and activity was discussed. 