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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (07): 1161-1164. 上一篇    下一篇

研究简报

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

习保民a; 江振洲b ; 王 涛b ; 倪沛洲*,c   

  1. (a南方医科大学药学院药物化学系 广州 510515)
    (b中国药科大学新药筛选中心 南京 210038)
    (c中国药科大学有机化学教研室 南京 210038)
  • 收稿日期:2008-11-22 修回日期:2009-02-21 发布日期:2009-07-22
  • 通讯作者: 倪沛洲

Synthesis and Biological Activity of Cyclosulfamido Substituted Phenylethylamine and Phenoxylalkylamine Derivatives

Xi, Baomina ; Jiang, Zhenzhou b; Wang, Tao b; Ni, Peizhou*,c   

  1. (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)
  • Received:2008-11-22 Revised:2009-02-21 Published:2009-07-22
  • Contact: Ni, Peizhou

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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

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-benzo[e][1,2]thiazine)hydrocholoride (5). Their structures were identified by 1H NMR, HRMS, and IR data. The target compounds have been assayed with function analysis in anococcyeus muscle, indicating that all of them have good blocking activity to α1-adrenoceptor.

Key words: synthesis, α1-adrenoceptor antagonist, sulfonamide