Schneider等曾报道,某些具有大环状结构氨基侧链的4-氨基喹啉类化合物对小鼠伯氏原虫(Plasmodium berghei)血症具有长效抑制作用。据称化合物12,278 R.P.(Ⅰ)—剂500mg/kg灌服,对小鼠伯氏原虫输血感染的有效保护期为8周。为了研究这类化合物的化学结构与抗疟作用的关系,作者设计合成了十种不同结构类型800余种哌嗪氨基氮杂环衍生物,研究结果表明HPQ(Ⅱ)是一种高 Schneider et al. Have reported that certain 4-aminoquinolines having amino side chains with macrocyclic structures have a long-term inhibitory effect on Plasmodium berghei hyperlipidemia. Alleged compound 12,278 R.P. (I) - agent 500mg / kg orally, the effective protection period of mice Bordetella transfusion infection for 8 weeks. In order to study the relationship between the chemical structure of these compounds and their anti-malarial effects, the authors designed and synthesized more than 800 piperazine amino nitrogen heterocyclic derivatives of ten different structural types. The results show that HPQ (II)