【摘要】 以97-9-G4为先导物,设计并合成一系列双哌嗪季铵盐,测定其镇痛活性,研究其构效关系。合成了8个双哌嗪季铵盐5a-h,测定了它们的体内镇痛活性,结果表明先导物97-9-G4中的苯乙基结构为必需的活性基团,苯环上引入吸电子基团有利于提高活性,苯环和哌嗪氮原子的距离为两个碳原子时镇痛活性最好。所合成的化合物具有一定的镇痛活性,但弱于先导化合物97-9-G4,总结出的构效关系对该类化合物的进一步结构修饰具有重要的指导意义。更多还原

【Abstract】 Selecting compound 97-9-G4 as lead compound,a series of bispiperazinium salts 5a-h were designed,synthesized and evaluated for their analgesic activities. The results show that phenylethyl group of 97-9-G4 is a crucial pharmacophore; the intro-duction of electron-withdrawing group on benzene ring is favorable to the activity.更多还原