摘要
将多种取代苯氧乙叉基团与3,4-二甲氧基苯乙胺结合,合成15个未见文献报道的苯乙胺型化合物,经波谱分析证实其结构。15个化合物的放射配基结合试验表明,大多数化合物对α_1-受体亲和力值在1μmol以下,其中化合物1-(4-甲氧基)-2-(3,4-二甲氧基苯乙胺基)丙烷盐酸盐可达9nmol·L^(-1),部分化合物对α_1-受体呈现了好的选择性,其IC_(50)(α_2/α_1)值大于100以上。对其中的5个化合物进行了实验性大鼠急性降压实验,均有不同程度的降压活性。根据化合物的活性,对其构效关系作了初步探讨,建立了相应的QSAR方程。
On the basis of the structural features, pharmacological effects of some well known compounds and the positive results obtained by our group, fifteen new compounds were designed and synthesized. Their structures have also been confirmed by spectroscopic elucidation. According to the preliminary pharmacological tests, the majority of the compounds show higher α-adrenocptor activity and potent antihypertensive activity. The structure-activity relationship of these compounds has been prilimilarily studied, and the results of the analysis may be useful to develop drug in future.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1992年第4期203-208,共6页
Journal of China Pharmaceutical University
关键词
苯乙胺
降压活性
构效关系
Benzylethylamine
α-Adrenocptors
Antihypertensive activity
Structure-activity relationship
