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８５７ｍｍｐＬ·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 H1, H11, H17, E1, E3 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 H7,15, E7 exerted significant inhibiting action toward 857 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 structureactivity relationships of this kind of aromatic amides are discussed herein.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第9期666-674,共9页
Acta Pharmaceutica Sinica
关键词
苯甲酰胺
扩血管活性
构效关系
合成
Benzamide
Vasodilativeactivity
Structureactivity relationships
