刘瑞武, 高由松, 张守仁, 梁晓天. 3,4-二氢-海南新碱类似物的合成及抗溃疡作用J. 药学学报, 1998, 33(9): 682-687.
引用本文: 刘瑞武, 高由松, 张守仁, 梁晓天. 3,4-二氢-海南新碱类似物的合成及抗溃疡作用J. 药学学报, 1998, 33(9): 682-687.
Liu Ruiw, Gao Yousong, Zhang Shouren , Liang Xiaotian, . SYNTHESIS AND ANTIULCER ACTIVITY OF 3,4-DIHYDRO-HAINANENSINE ANALOGSJ. Acta Pharmaceutica Sinica, 1998, 33(9): 682-687.
Citation: Liu Ruiw, Gao Yousong, Zhang Shouren , Liang Xiaotian, . SYNTHESIS AND ANTIULCER ACTIVITY OF 3,4-DIHYDRO-HAINANENSINE ANALOGSJ. Acta Pharmaceutica Sinica, 1998, 33(9): 682-687.

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

  • 摘要: 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。对构效关系进行了初步分析。

     

    Abstract: 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. 

     

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