A series of short chain 4-aminoquinoline-imidazole derivatives have been synthesized in one pot two step multicomponent reaction using van leusen standard protocol. The diethylamine function of chloroquine is replaced by substituted imidazole derivatives containing tertiary terminal nitrogen. All the synthesized compounds were screened against the chloroquine sensitive (3D7) and chloroquine resistant (K1) strains of Plasmodium falciparum. Some of the compounds (6, 8, 9 and 17) in the series exhibited comparable activity to CQ against K1 strain of P. falciparum. All the compounds displayed resistance factor between 0.09 and 4.57 as against 51 for CQ. Further, these analogues were found to form a strong complex with hematin and inhibit the β-hematin formation, therefore these compounds act via heme polymerization target.

使用van leusen标准规程，通过一锅两步多组分反应合成了一系列短链4-氨基喹啉-咪唑衍生物。氯喹的二乙胺官能团被取代的含叔末端氮的咪唑衍生物取代。针对恶性疟原虫的氯喹敏感性（3D7）和耐氯喹（K1）菌株筛选了所有合成的化合物。一些化合物（的6，8，9和17中的系列）表现出相当的活性，以针对CQ的K1株恶性疟原虫。所有化合物均显示出0.09至4.57的电阻系数，而CQ为51。此外，发现这些类似物与血红素形成强复合物并抑制β-血红素的形成，因此这些化合物通过血红素聚合靶起作用。