摘要
目的:合成含噻二唑噁二唑双杂环的槟榔碱衍生物,研究目标化合物体外舒张血管活性。方法:将化合物1a～e的吡啶环用碘甲烷季铵化得到相应的季铵盐,用NaBH4还原季铵盐得到目标物3a～e。采用离体血管条法研究目标化合物体外舒张血管活性。结果:合成了5个槟榔碱衍生物,目标化合物的结构经元素分析、IR、1HNMR、MS确证。在10μmol/L浓度下,化合物3a、3b、3c、3d、3e对离体血管舒张率分别为17.06%,27.35%,31.36%,27.32%和21.74%,在相同的条件下.槟榔碱的舒张率为21%。结论:噻二唑噁二唑双杂环可以作为槟榔碱酯基的生物电子等排体。
Objective：To synthesize Arecoline Analogues Containing Diheterocyclic of Triazole and Oxodiazole,and the in vitro vascular relaxing activity of target compounds.Methods：The pyridine ring of the compound 1a ～e was quaternized with methyl iodide to afford the corresponding methylpyridiniun salts,and reducted the methylpyridiniun salts with sodium borohydride to give a series of the corresponding target compounds 3a ～e.The in vitro vascular relaxing activity of target compounds were screened.Results：Five Arecoline Analogues were synthesized.The structures of the synthesized compounds were characterized by IR,H NMR,MS spectra and element analysis.At the concentration of 10μ mol/L,their vascular relaxing effects on isolated endothelial cells were 17.06%,27.35%,31.36%,27.32%and 21.74%.while arecoline as reference drug was 21% at the same conditions.Conclusion：The Diheterocyclic of Triazole and Oxodiazole can be bioisosterism of the ester group of arecoline.
出处
《泸州医学院学报》
2010年第2期157-159,共3页
Journal of Luzhou Medical College
关键词
槟榔碱衍生物
噻二唑
噁二唑
舒张血管活性
合成
Arecoline derivatives
Thiadiazole
Oxodiazole
Vascular relaxing activity
Synthesis
