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在二哌喹(Ⅰ)类化合物的中间碳链结构与抗疟作用关系研究的基础上,我们设计合成了两类新的哌喹型化合物:烷氨基二哌喹(Ⅱ)和四哌喹(Ⅲ)。经鼠疟抑制性初筛,所合成的此二类化合物其抗疟活性并不高于哌喹。它们的实验数据见表1。实验部分一、7-氯-4-(γ-羟丙基)氨基噎啉的制备参照Elderfield等的方法,由氨基醇与4,7-二氯喹啉反应制得。7-氯-4-(β-羟乙基)氨基喹啉的收率为94％,熔点214.5～216.5℃;7-氯-4-(γ-羟丙基)氨基喹啉的收率为91.33％,熔点153～154℃。
Based on the study of the relationship between the intermediate carbon chain structure of dipipequine and the anti-malarial effect, we designed and synthesized two novel piperazinyl compounds: alkylamino-dipipequine (Ⅱ) and tetra-piperazine Ⅲ). The inhibitory screening of murine malaria, the two compounds synthesized anti-malarial activity is not higher than that of piperaquine. Their experimental data in Table 1. Experimental Part I. Preparation of 7-chloro-4- (γ-hydroxypropyl) aminophenanthroline According to the method of Elderfield et al., It is prepared by the reaction of amino alcohol and 4,7-dichloroquinoline. The yield of 7-chloro-4- (β-hydroxyethyl) aminoquinoline was 94% and the melting point was 214.5-216.5 ° C. The yield of 7-chloro-4- (γ- hydroxypropyl) aminoquinoline was 91.33 %, Mp 153-154 ° C.