Microwave promoted high yielding synthesis of 4-aminoquinoline-phthalimides was developed with an aim to evaluate their anti-plasmodial potential. The scaffolds with longer spacer length (n = 6, 8) between two pharmacophores and a halogen substituent on the phthalimide ring displayed good antiplasmodial activity. Compound 5w, with an optimum combination of hexyl chain as spacer along with a tetra-bromophthalimide ring proved to be most potent and non-cytotoxic among the series exhibiting an IC₅₀ value of 0.10 μM.

中文翻译：

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微波促进的4-氨基喹啉-邻苯二甲酰亚胺的合成：合成和抗疟原虫评估

微波促进高产合成4-氨基喹啉-邻苯二甲酰亚胺的目的是评估其抗疟原虫的潜力。在两个药效基团之间具有更长的间隔区长度（n = 6、8）且邻苯二甲酰亚胺环上的卤素取代基的支架显示出良好的抗血浆活性。在具有IC ₅₀值为0.10μM的系列中，具有己基链作为间隔基与四溴邻苯二甲酰亚胺环的最佳组合的化合物5w被证明是最有效且无细胞毒性的化合物。