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临床验证常咯啉(Ⅰ)对短阵室性心动过速和室性早搏等症状非常有效,但存在一些副作用。为了寻找优于常咯啉的新的抗心律失常药物,我们合成了一系列芳环或芳杂环的Mannich:碱化合物37个。化合物的制备系将各类相应的氯化物分别与对氨基酚缩合,所得的中间体再与甲醛及胺反应,得到预期的Mannich碱(列于表2～表4)。药理试验结果表明。化合物9,12,13,30和33均能对抗乌头碱型实验性心律失常,其中化合物9,12和13的作用较强,安全范围较大。药理结果将另文发表。
Clinical verification of regular pyrroline (Ⅰ) is very effective in the treatment of symptoms of paroxysmal ventricular tachycardia and ventricular premature beats, but there are some side effects. In order to find new anti-arrhythmic drugs superior to those of statin, we synthesized a series of aromatic or heteroaromatic Mannich: 37 base compounds. The compounds were prepared by condensing the corresponding chlorides with p-aminophenol respectively. The resulting intermediates were reacted with formaldehyde and amines to give the expected Mannich bases (Table 2 to Table 4). Pharmacological test results show. Compounds 9, 12, 13, 30, and 33 were able to combat aconitine-type experimental arrhythmias, with compounds 9, 12 and 13 being more potent and safe. Pharmacological results will be published separately.