作为潜在抗高血压药物的四氢-1,4-苯并二氮杂䓬衍生物。
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
作者信息
Kim D H
出版信息
J Med Chem. 1977 Feb;20(2):209-12. doi: 10.1021/jm00212a005.
4-Amidino derivatives and quaternary salts of tetrahydro-1,4-benzodiazepines were synthesized and evaluated for antihypertensive activity in conscious rats by the oral route. Included in this study were derivatives of 1,2,4,5,6,7-hexahydropyrrolo[3,2,1-jk][1,4]benzodiazepine and 1,2,3,4,8,9,10,11-octahydro[1,4]diazepino[6,5,4-jk]carbazole in which the 1 and 9 positions of tetrahydro-1,4-benzodiazepine are linked by an ethylene and a cyclohexenyl chain, respectively. Four compounds exhibited marked blood pressure lowering activity (greater than 50 mmHg) at doses of 75 mg/kg. Further study indicated that these compounds are effective by impairing transmission in the sympathetic nervous system.
合成了四氢-1,4-苯二氮䓬的4-脒基衍生物和季铵盐，并通过口服途径在清醒大鼠中评估其抗高血压活性。本研究包括1,2,4,5,6,7-六氢吡咯并[3,2,1-jk][1,4]苯二氮䓬和1,2,3,4,8,9,10,11-八氢[1,4]二氮杂䓬并[6,5,4-jk]咔唑的衍生物，其中四氢-1,4-苯二氮䓬的1位和9位分别通过乙烯链和环己烯基链相连。四种化合物在75mg/kg剂量下表现出显著的降压活性（大于50mmHg）。进一步研究表明，这些化合物通过损害交感神经系统的传递而发挥作用。
Zotero 插件