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

摘要/Abstract

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

引用此文

赵圣印,黄文龙. 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[J]. 有机化学, 2008, 28(2): 240-245.

ZHAO Sheng-Yin*^,a,b,HUANG Wen-Long^a. Synthesis and Vasorelaxant Activity of N-(3,4-Dihydro-2H-1-ben- zopyran-4-yl)isothiourea Derivatives as K^＋ Channel Openers[J]. Chin. J. Org. Chem., 2008, 28(2): 240-245.

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