何欣, 林紫云, 朱莉亚, 付焕建. 苯甲酰胺类衍生物的合成及扩血管活性J. 药学学报, 1998, 33(9): 666-674.
引用本文: 何欣, 林紫云, 朱莉亚, 付焕建. 苯甲酰胺类衍生物的合成及扩血管活性J. 药学学报, 1998, 33(9): 666-674.
He Xin, Lin Ziyun, Zhu Liya , Fu Huanjian, . SYNTHESIS AND VASODILATIVE ACTIVITIESOF BENZAMIDE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1998, 33(9): 666-674.
Citation: He Xin, Lin Ziyun, Zhu Liya , Fu Huanjian, . SYNTHESIS AND VASODILATIVE ACTIVITIESOF BENZAMIDE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1998, 33(9): 666-674.

苯甲酰胺类衍生物的合成及扩血管活性

SYNTHESIS AND VASODILATIVE ACTIVITIESOF BENZAMIDE DERIVATIVES

  • 摘要: 报道了22个苯甲酰胺类衍生物的合成,其中大多数化合物有不同程度的扩血管活性,化合物H1,11,17,E1,3对去甲肾上腺素NE(10-7mol·L-1)引起的大鼠主动脉条收缩的抑制作用明显优于先导物N-(4-甲氧基苯甲酰基)-N′-肉桂基哌嗪,化合物H7,15,E7对85.7mmpL·L-1KCl引起的大鼠主动脉条收缩有明显的抑制作用,进一步钾通道实验表明E1可能为ATP敏感型钾通道开放剂。并初步分析了此类化合物的构效关系。

     

    Abstract: Twenty two benzamide derivatives were synthesized of which twenty one were not reported before. Vasodilative activity screening in vitro has shown that most of the compounds possess various activities, among which compound H1, H11, H17, E1, E3 demonstrated a superior pharmacological profile to the lead compound when inhibiting effect on the noradrenaline (10-7mol·L-1) induced contraction of rat aortic strip was chosen as the evaluation criterion, while H7,15, E7 exerted significant inhibiting action toward 85.7 mmol·L-1 KCl induced contraction of rat aortic strip. Further evaluation assays for their KCO potentials showed that E1 might be an ATP sensitive KCO. Preliminary structureactivity relationships of this kind of aromatic amides are discussed herein.

     

/

返回文章
返回