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

A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized and assessed as an-timalarial 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. Com-pound 5n showed the monoclinic crystal system and P21 space group. Compounds 5a -5m all exhibited good inhibitory activities associated with beta-hematin formation. Compound 5c had the best inhibitory activity of beta-hemotin formation with IC50 values of 4.54 +/- 0.16 mu M.(c) 2022 Elsevier B.V. All rights reserved.

Automated summary

A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized, and evaluated as antimalarial agents. The structures of these hybrids were confirmed, and compound 5c exhibited the best inhibitory activity.