苯甲酰胺类衍生物的合成及扩血管活性  

SYNTHESIS AND VASODILATIVE ACTIVITIESOF BENZAMIDE DERIVATIVES

作　　者：何欣[1] 林紫云[1] 朱莉亚[1] 付焕建[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所

出　　处：《药学学报》1998年第9期666-674,共9页Acta Pharmaceutica Sinica

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。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 H1, H11, H17, E1, E3 demonstrated a superior pharmacological profile to the lead compound when inhibiting effect on the noradrenaline (10-7 mol·L-1) induced contraction of rat aortic strip was chosen as the evaluation criterion, while H7,15, E7 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 E1 might be an ATP sensitive KCO. Preliminary structureactivity relationships of this kind of aromatic amides are discussed herein.

关 键 词：苯甲酰胺 扩血管活性 构效关系 合成 

分 类 号：TQ463.26[化学工程—制药化工] R872.4[医药卫生—运动医学]