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

• Published in: Journal of molecular structure Vol. 1271; p. 133982
• Main Authors: Feng, Yuan-Yuan, Dong, Chang-E, Li, Rui, Zhang, Xiao-Qing, Wang, Wei, Zhang, Xing-Rui, Liu, Wei-Wei, Shi, Da-Hua
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 05.01.2023
• Subjects: Malaria; Quinoline; Triazine; β-hematin; Quinoline; Triazine; β-hematin; Malaria
• ISSN: 0022-2860; 1872-8014
• DOI: 10.1016/j.molstruc.2022.133982

•Fifteen quinoline-1,2,4-triazine hybrids were designed and synthesized.•New compounds were confirmed by different spectral techniques and X-ray crystallographic analysis.•Compound 5c exhibited the best β-hematin formation inhibitory activity with IC50 values of 4.54 ± 0.16 µM. 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 IC50 values of 4.54 ± 0.16 µM. [Display omitted]