【摘要】 为寻找高效、低毒的抗心律失常新药,以关附甲素为先导物进行结构修饰,设计合成了6个化合物。初步药理实验结果表明,化合物Ⅰ、Ⅱ和Ⅵ对乌头碱诱发大鼠心律失常具有明显的保护作用。更多还原

【Abstract】 Guanfu base A (GFA) ia an alkaloid isolated from the root of Aconitum coreanum and is effective in several experimental arrhythmic models. Thus, GFA was chosen as a lead compound for chemical modification. Six ester derivatives of Guanfu alcohol-amine (AA) were synthesized by acylating AA or GFA and their structures were confirmed by IR, MS and elemental analysis. Preliminary pharmacological study showed that compound Ⅰ, Ⅱ and Ⅵ were effective against aconitine-induced arrhythmia in rats.更多还原