Mastomys natalensis. The most active antimalarial compound, 7-chloro-4-[alpha-[[N-(4-methyl-1-piperazinyl)carbonyl]amino]-4-hydroxy-m-toluidino]quinoline, had twice the activity of amodiaquine. O-Methylation and N-ethylation generally reduced antimalarial activity. Analogues which lack a basic tertiary amino function at their side chain were also lacking in both antimalarial and antifilarial activities.
设计并合成了十个
氨二喹类似物,它们是
氨二喹和
二乙基氨基甲嗪的杂交分子。六种类似物均在其侧链上具有基本的叔
氨基功能,它们在小鼠中对伯氏疟原虫具有活性,并在体外抑制成虫的活动性和Breinlia booliati的微丝虫。它们对纳塔氏乳杆菌中的Litomosoides carinii没有活性。最具活性的抗疟疾化合物7-
氯-4- [α-[[N-(4-甲基-1-
哌嗪基)羰基]
氨基] -
4-羟基-间
甲苯基]
喹啉的活性是
氨二喹的两倍。O-甲基化和N-乙基化通常会降低抗疟活性。在其侧链上缺乏基本叔
氨基功能的类似物在抗疟和抗孝活性上也都缺乏。