3,4-二氢海南粗榧碱类似物的合成及其抗溃疡活性
[Synthesis and antiulcer activity of 3,4-dihydro-hainanensine analogs].
作者信息
Liu R, Gao Y, Zhang S, Liang X
机构信息
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
出版信息
Yao Xue Xue Bao. 1998 Sep;33(9):682-7.
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.
为了寻找具有新作用模式、高抗溃疡活性和低毒性的新化合物，合成了26种（13对对映异构体A和B）3,4-二氢哈那宁类似物。所有化合物均在M1受体结合试验和大鼠冷浸应激诱导的胃溃疡模型中进行了测试。大多数化合物表现出抗溃疡活性，其中IX3A、IX7A、IX8A、IX12A、IX12B和IX13A表现出比对照化合物西咪替丁更强的抗溃疡活性。同时，讨论了它们的结构与活性之间的关系。
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