Chin. J. Org. Chem. ›› 2009, Vol. 29 ›› Issue (07): 1161-1164. Previous Articles     Next Articles

Reports

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 出版日期:2009-07-22 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 Online:2009-07-22 Published:2009-07-22
  • Contact: Ni, Peizhou

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