A series of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline, and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives was designed, synthesised, and evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, and Trypanosoma brucei brucei). Biological results showed antiprotozoal activity with IC₅₀ values in the µM range. In addition, the in vitro cytotoxicity of these original molecules was assessed with human HepG2 cells. The quinoline 1c was identified as the most potent antimalarial candidate with a ratio of cytotoxic to antiparasitic activities of 97 against the P. falciparum CQ-sensitive strain 3D7. The quinazoline 3h was also identified as the most potent trypanosomal candidate with a selectivity index (SI) of 43 on T. brucei brucei strain. Moreover, as the telomeres of the parasites P. falciparum and Trypanosoma are possible targets of this kind of nitrogen heterocyclic compounds, we have also investigated stabilisation of the Plasmodium and Trypanosoma telomeric G-quadruplexes by our best compounds through FRET melting assays.

一系列新的2,4-双[（取代的氨基甲基）苯基]喹啉，1,3-双[（取代的氨基甲基）苯基]异喹啉和2,4-双[（取代的氨基甲基）苯基]喹唑啉衍生物设计，合成和体外针对三种原生动物寄生虫（恶性疟原虫，利什曼原虫donovani和布氏锥虫布鲁氏菌）进行了评估。生物学结果显示了抗原生动物活性，IC ₅₀值在µM范围内。另外，用人类HepG2细胞评估了这些原始分子的体外细胞毒性。喹啉1c被鉴定为最有效的抗疟疾候选药物，对恶性疟原虫CQ敏感菌株3D7的细胞毒性与抗寄生虫活性之比为97 。喹唑啉3h也被确定为最有效的锥虫候选物，对布鲁氏布鲁氏菌菌株的选择性指数（SI）为43 。此外，由于寄生虫恶性疟原虫和锥虫的端粒是这类氮杂环化合物的可能靶标，我们还通过FRET熔解法通过我们最好的化合物研究了疟原虫和锥虫端粒G-四链体的稳定性。