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| 环状胺磺酰基取代的苯乙胺和苯氧烷胺衍生物的合成及生物活性测试 | |
| 引用本文： | 习保民,江振洲,王涛,倪沛洲.环状胺磺酰基取代的苯乙胺和苯氧烷胺衍生物的合成及生物活性测试[J].有机化学,2009,29(7):1161-1164. |
| 作者姓名： | 习保民 江振洲 王涛 倪沛洲 |
| 作者单位： | 1. 南方医科大学药学院药物化学系,广州,510515 2. 中国药科大学新药筛选中心,南京,210038 3. 中国药科大学有机化学教研室,南京,210038 |
| 基金项目： | 国家自然科学基金，国家高技术研究发展计划(863计划) |
| 摘 要： | 7-氨基乙基-(3,4-二氢-2H-苯并1,2]噻嗪-1,1-二氧代)盐酸盐和取代苯氧丙-2-酮经还原胺化, 合成了10个新的环状胺磺酰基取代的苯乙胺和苯氧烷胺类化合物. 化合物经1H NMR, HRMS, IR确证其结构. 生物活性测试结果表明, 所有化合物对α1-肾上腺素受体均具有一定的拮抗作用. |
| 关 键 词： | 磺酰胺 合成 α1-肾上腺素受体拮抗剂 |
| 收稿时间： | 2008-11-22 |
| 修稿时间： | 2009-2-21 |
Synthesis and Biological Activity of Cyclosulfamido Substituted Phenylethylamine and Phenoxylalkylamine Derivatives |
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| Xi, Baomin,Jiang, Zhenzhou,Wang, Tao,Ni, Peizhou.Synthesis and Biological Activity of Cyclosulfamido Substituted Phenylethylamine and Phenoxylalkylamine Derivatives[J].Chinese Journal of Organic Chemistry,2009,29(7):1161-1164. | |
| Authors: | Xi Baomin Jiang Zhenzhou Wang Tao Ni Peizhou |
| Institution: | (a Department of Medicinal Chemistry, College of Pharmacy, Southern Medical University, Guangzhou 510515) (b National Drug Screening Center, China Pharmaceutical University, Nanjing 210038) (c Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210038) |
| Abstract: | A series of novel cyclosulfamido substituted phenoxylalkylamine derivatives were synthesized through the condensation and reduction of various substituted phenoxypropan-2-one with 7-(2-aminoethyl-3,4-dihydro-1,1-dioxo-2H-benzoe]1,2]thiazine)hydroeholoride (5). Their structures were identified by 1H NMR, HRMS, and IR data. The target compounds have been assayed with function analysis in anococeyeus muscle, indicating that all of them have good blocking activity to α1-adrenoceptor. |
| Keywords: | sulfonamide synthesis |
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