苯并吡喃-4-硫脲类化合物的合成及其血管舒张活性  

Synthesis and Vasorelaxant Activity of Benzopyran-4-thioureas

作　　者：赵圣印[1] 黄文龙[1] 

机构地区：[1]中国药科大学新药研究中心

出　　处：《合成化学》2007年第1期30-33,共4页Chinese Journal of Synthetic Chemistry

摘　　要：根据苯并吡喃类钾通道开放剂的作用机理和构效关系,合成了4个新的苯并吡喃-4-硫脲类化合物(3a^3d),其结构经1HNMR,IR,MS和元素分析确证。大鼠体外血管扩张实验结果表明,3(1.0×10-5mol·L-1)对30mmol·L-1KCl诱导的大鼠主动脉条收缩均具有一定程度的抑制作用,其中3a的血管收缩抑制活性较强。In search of more potent, less toxic and selective potassium channel openers, four novel benzopyran-4-thiourea derivatives（3a～3d） were synthesized and evaluated for vasorelaxant activity against 30 mmol·L^-1 KCl inducing contraction of rat aorta in vitro. The structures of 3a～ 3d were confirmed by ^1H NMR, IR, MS and elemental analysis. The preliminary bioassay suggested that these compounds exhibited some, but less vasorelaxant activity than Emakalim on the concentration of 1.0×10^-5 mol·L^-1.

关 键 词：苯并吡喃 钾通道开放剂 合成 血管舒张活性 

分 类 号：R914.5[医药卫生—药物化学] O625.63[医药卫生—药学]