【作者】 高宁星；

【导师】 王国清；

【作者基本信息】 沈阳药科大学 ， 药物化学， 2002， 硕士

【摘要】 本文概述了消化系统溃疡的多种发病机理及药物研究现状，依照联合不同作用方式寻找药物的思路，设计了具有双重抗溃疡作用的H₂受体拮抗剂与锌盐的配合物。通过H₂受体拮抗剂与锌反应，形成多元配合物，合成了19个化合物，其中14个未见文献报道，并经过元素分析、红外、紫外、热分析及X-射线衍射对其结构进行了确证。 对自制的H₂受体拮抗剂锌盐配合物进行了初步的药效学研究，试验结果表明，所合成的化合物绝大部分对乙醇及阿司匹林诱发小鼠胃溃疡显示出明显的抑制溃疡形成作用或粘膜保护作用。所合成的配合物中C-04、C-05、C-10、C-11的粘膜保护活性显著高于西米替丁，另外R-01、R-04、R-05、F-02、F-03的活性亦高于同系列的标准对照药。更多还原

【Abstract】 This paper reviewed the pathogenesis of digestive ulcer and clinical application of anti-ulcer medicines. Based on the combine theory, a series of double anti-ulcer function complexes of Histamine H₂-Receptor Antagonists and Zinc were designed and synthesized.Through the complexation of H₂-Receptor Antagonists and salt of Zinc, nineteen binary or triple center complexes were synthesized in the paper. Of them .fourteen compound have not been reported hi literature. Their structures were identified by IR, UV, TG-DTA, X-ray and as well as titration and elementary analysis.As a result of the preliminary pharmacodynamic experiments, most of the complexes showed significant anti-ulcer and cytoprotective activity against stomach ulcer of mice respectively induced by absolute alcohol and aspirin. Among them , the ulcer exhibition activity of complex C-04,C-05,C-10,C-11 is obviously stronger than cimetidine , and the activity of complex R-01 , R-04, R-05, F-02 , F-03 is also much stronger than their contrast medicine.更多还原