|
|||||
|
|
| 阿齐利特类似物的合成及其抗心律失常活性研究 | |
| 引用本文： | 郑其萍,丰艳梅,颜战胜. 阿齐利特类似物的合成及其抗心律失常活性研究[J]. 中国药物化学杂志, 2009, 19(1) |
| 作者姓名： | 郑其萍 丰艳梅 颜战胜 |
| 作者单位： | 1.西安市铁路中心医院 药剂科，陕西 西安 710054；2. 西安交通大学 医学院 第二附属医院， 陕西 西安 710004； 3. 陕西省雄风制药有限公司， 陕西 渭南 714000 ;; |
| 摘 要： | 目的 设计合成阿齐利特类似物，并研究其体外抗心律失常活性。方法 以1-氨基海因盐酸盐(1)为原料，1与一系列醛进行缩合反应得到关键中间体1-(取代甲叉基)氨基海因(2)；2与1,4-二溴丁烷或1,3-二溴丙烷反应生成3，3与一系列仲胺反应，再经成盐得到盐酸阿齐利特衍生物。结果 设计合成了未见文献报道的12个目标化合物，所有化合物均经过1H-NMR谱及MS谱确证。结论 目标化合物5b、5h、5i、5j对离体心肌细胞具有III类抗心律失常药物延长动作电位时程的特征，其中化合物5h活性最好。 |
| 关 键 词： | 阿齐利特；抗心律失常活性；类似物；合成 |
| 收稿时间： | 2008-06-17 |
| 修稿时间： | 2008-05-05 |
Synthesis and antiarrhythmic activity of azimilide analogues |
|
| ZHENG Qi-ping,FENG Yan-mei,YAN Zhan-sheng. Synthesis and antiarrhythmic activity of azimilide analogues[J]. Chinese Journal of Medicinal Chemistry, 2009, 19(1) | |
| Authors: | ZHENG Qi-ping FENG Yan-mei YAN Zhan-sheng |
| Affiliation: | 1. Department of Pharmacy, Xi’an Railway CentralHospital, Xi’an 710054, China; 2. The Second Affiliated Hospital, Medical College of Xi’an Jiaotong University, Xi’an 710004, China; 3. Shanxi Xiongfeng Pharmaceutical Corporation, Weinan 714000, China |
| Abstract: | Aim To design and synthesize azimilide analogues and to investigate their antiarrhythmic activities in vitro. Methods 1-(Substituted)aminohydantoins(2) was obtained by condensation of 1-aminohydantoin hydrochloride(1) and a series of aldehyde. 1-(Substituted)amino-3-(4-bromobutyl) hydantoins(3) was obtained by reaction of 2 with 1,4-dibromobutane or 1,3-dibromopropane. Target compounds were obtained by reaction of 3 with a series of substituted secondary amine, then salt formation. Result All of the title compounds were confirmed by 1H-NMR and MS spectra, respectively. Conclusion Compounds 5b, 5h, 5i, 5j have antiarrhythmic activity, especially compound 5h. |
| Keywords: | azimilide antiarrhythmic activity analogues synthesis |
| 点击此处可从《中国药物化学杂志》浏览原始摘要信息 | |
| 点击此处可从《中国药物化学杂志》下载全文 | |