有机化学 ›› 2008, Vol. 28 ›› Issue (2): 240-245. 上一篇    下一篇

研究论文

N-(3,4-二氢-2H-1-苯并吡喃-4)异硫脲类化合物的合成及其血管舒张活性

赵圣印*,a,b,黄文龙a   

  1. (a中国药科大学新药研究中心 南京 210009)
    (b东华大学化学与化工学院 上海 201620)
  • 收稿日期:2007-01-04 修回日期:2007-08-30 发布日期:2008-02-01
  • 通讯作者: 赵圣印

Synthesis and Vasorelaxant Activity of N-(3,4-Dihydro-2H-1-ben- zopyran-4-yl)isothiourea Derivatives as K Channel Openers

ZHAO Sheng-Yin*,a,b,HUANG Wen-Longa   

  1. (a New Drug Research Center, China Pharmaceutical University, Nanjing 210009)
    (b College of Chemistry and Chemical Engineering, Donghua University, Shanghai 201620)
  • Received:2007-01-04 Revised:2007-08-30 Published:2008-02-01
  • Contact: ZHAO Sheng-Yin

根据苯并吡喃类钾通道开放剂的作用机理和构效关系, 设计合成了13个苯并吡喃-4-异硫脲衍生物, 其结构经IR, 1H NMR, MS和元素分析确证. 大鼠体外血管扩张实验研究表明, 多数化合物在1×10-5 mol•L-1 浓度下对30 mmol•L-1 KCl诱导的大鼠主动脉条收缩具有一定程度的抑制作用, 其中化合物6l的血管收缩抑制活性较强.

关键词: N-(3,4-二氢-2H-1-苯并吡喃-4)异硫脲, 钾通道启开剂, 血管舒张活性

In search of more potent, less toxic and selective potassium channel openers, thirteen N-(3,4- dihydro-2H-1-benzopyran-4-yl)isothiourea derivatives were synthesized and evaluated for vasorelaxant activity against 30 mmol•L-1 KCl inducing contraction of rat aorta in vitro. Their structures were confirmed by spectral data and elemental analysis. The preliminary bioassay suggested that these compounds exhibited some vasorelaxant activities at a con-centration of 1×10-5 mol•L-1. The compound 6l also showed a good vasorelaxant activities at a 1×10-6 mol•L-1 concentration.

Key words: potassium channel opener, N-(3,4-dihydro-2H-1-benzopyran-4-yl)isothiourea, vasorelaxant activity