Design, synthesis and biological evaluation of quinoline-1,2,4-triazine hybrids as antimalarial agents

Summary A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized and assessed as antimalarial agents. The structures of the 1,2,4-triazine-quinoline hybrids were confirmed by IR, NMR, HRMS and single-crystal X-ray diffraction studies. Compound  5f  had the crystal system of monoclinic and  Cc  space group. Compound  5j  possessed the monoclinic crystal system and  C2/c  space group. Compound  5n  showed the monoclinic crystal system and  P21  space group. Compounds 5a - 5m all exhibited good inhibitory activities associated with β -hematin formation. Compound 5c had the best inhibitory activity of β -hemotin formation with IC 50 values of 4.54 ± 0.16 µM.