| 2,4-二甲氧基苯乙胺类α1-肾上腺素受体拮抗剂的合成、生物活性研究 |
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| 引用本文： | 习保民,江振洲,王涛,倪沛洲.2,4-二甲氧基苯乙胺类α1-肾上腺素受体拮抗剂的合成、生物活性研究[J].中国药物化学杂志,2008,18(6):401-405. |
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| 作者姓名： | 习保民 江振洲 王涛 倪沛洲 |
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| 作者单位： | (1. 南方医科大学 药学院 药物化学系，广东 广州 510515； 2. 中国药科大学 国家新药筛选中心，江苏 南京 210038；3. 中国药科大学 有机化学教研室，江苏 南京 210009) |
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| 基金项目： | 国家自然科学基金项目（30600776）;国家高技术研究发展计划项目（863项目,2002AA2Z3118）. |
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| 摘 要： | 目的设计合成苯乙胺类α1-肾上腺素受体（α1-AR）拮抗剂,并研究它们对大鼠肛尾肌收缩功能的影响。方法以DDPH为先导化合物设计合成了11个新化合物,以2,6-二甲基苯酚为原料经多步反应得中间体卤代苯氧丙酮,再经还原胺化得目标物。运用大鼠肛尾肌收缩功能实验测定目标物的拮抗活性。结果共合成了11个目的物,其结构经IR、HRMS1、H-NMR确证。结论生物活性测试显示大部分目标化合物均具有一定的α1-AR拮抗活性,化合物Ⅲk拮抗作用和DDPH接近。
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| 关 键 词： | 化学合成 α1-AR拮抗剂 DDPH |
| 收稿时间： | 2008-6-10 |
| 修稿时间： | 2008-9-20 |
Study on the synthesis, biological activity of 2,4-dimethoxyphenylethylamines as α1-AR antagonist |
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| XI Bao-min,JIANG Zhen-zhou,WANG Tao,NI Pei-zhou.Study on the synthesis, biological activity of 2,4-dimethoxyphenylethylamines as α1-AR antagonist[J].Chinese Journal of Medicinal Chemistry,2008,18(6):401-405. |
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| Authors: | XI Bao-min JIANG Zhen-zhou WANG Tao NI Pei-zhou |
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| Institution: | (1. Department of Medicinal Chemistry, College of Pharmacy, Southern Medical University, Guangzhou 510515, China; 2. National Drug Screening Laboratory, China Pharmaceutical University, Nanjing 210038, China; 3. Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210009, China ) |
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| Abstract: | Abstract: Aim To study the blocking activity of 2,4-dimethoxyphenylethylamine analogues as α1-adrenocepter (α1-AR) antagonist. Methods Based on the biological activity of DDPH, 11 analogues of 2,4-dimethoxyphylethylamines were designed and prepared. The target compounds were synthesized from 2,6-dimethylphenol; their structures were confirmed by HRMS, 1H-NMR, IR spectra. Their bioactivities were also tested. Results The test indicate that most the target compounds exhibited well in blocking α1-adrenoceptor. Conclusion The preliminary bioassay indicates compound Ⅲk function well in blocking α1-adrenoceptor. |
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| Keywords: | Key word: chemical synthesis α1-adrenoceptor antagonist DDPH |
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