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根据关附甲素(GFA)结构特点设计合成11个(苏)-苯丙二醇胺类化合物(Ⅰ_(1～5) Ⅱ_(1～6)),其中8个未见文献报道(Ⅰ_(4～5) Ⅱ_(1～6))。经乌头碱诱发大鼠心律失常试验,筛选出8个化合物具有一定的抗心律失常活性,其中Ⅰ_1和Ⅰ_4活性与GFA相近。结果显示,化合物1结构中苯环对位引入硝基对抗心律失常活性不利。
According to the structure of Guanfu A (GFA), 11 compounds (Ⅰ - (1-5) Ⅱ 1-6) were designed and synthesized, of which 8 were not reported (Ⅰ ~ (4 ~ 5) Ⅱ_ (1 ~ 6)). The rat arrhythmia induced by aconitine test, screening out eight compounds have anti-arrhythmic activity, of which Ⅰ_1 and Ⅰ_4 activity and GFA similar. The results showed that the introduction of the para-position of the benzene ring in the structure of compound 1 was unfavorable for anti-arrhythmic activity.