节点文献
抗心律失常药物的研究——Ⅰ.3,4,5-三甲氧基苯甲酰胺衍生物的合成
STUDIES ON ANTIARRHYTHMICS Ⅰ.SYNTHESIS OF 3,4,5-TRIMETHOXYBENZAMIDE DERIVATIVES
【摘要】 <正> 心律失常是心血管疾病中最为常见的疾病之一。目前临床上应用的抗心律失常药奎尼丁、普鲁卡因胺、利多卡因、苯妥英钠、β-受体阻滞剂以及近年来出现的茚丙胺(Aprindine)等,均存在一定的缺点。为了寻找新的抗心律失常药,我们对普鲁卡因胺(1)、利多卡因(2)、室安卡因(Focainide)(3)、双异丙吡胺(Disopyramide)(4)、茚丙胺(5)、安他心(Antazoline)(6)、新安替根(Mepyramine)(7)和钙离子拮抗剂3,4,5-三甲氧基苯甲酸ω-二烷基胺基烷(C2~C8)酯(8)等抗心律失常药的化学结构进行了分析比较,综合这些药物
【Abstract】 Three 3,4,5-trimethoxybenzanilide derivatives (Ⅰ_a-Ⅰ_c) and two 3,4,5-trimethoxy-benzamides (Ⅰ_d-Ⅰ_c)were synthesized by condensing 3,4,5-trimethoxybenzoyl chloride with corresponding substituted ethylenediamines. Pharmacblogical tests showed that com-pounds Ⅰ_a, Ⅰ_b and Ⅰ_c exhibited significant antiarrhythmic activity. The therapeutic indices of Ⅰ_a, Ⅰ_b, Ⅰ_c and lidocaine in rats. against aconitine were 7.0, 7.4, 22.6 and 2.6, respectively. The therapeutic doses of Ⅰ_c and lidocaine in dogs against ouabain given intravenously were 10 mg/kg and 18.1 mg/kg respectively.
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1981年02期
- 【被引频次】7
- 【下载频次】94