4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents

A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line. Five compounds (19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg × 4 days against CQ-resistant strain of P. yoelii. Inhibition of β-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds.

A series of novel hybrid class 4-anilinoquinoline triazines have been synthesized and screened for their antimalarial activity in in vitro and in vivo assay.Figure optionsDownload as PowerPoint slideResearch highlights
► A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum.
► Five compounds (19, 20, 23, 41 and 45) exhibited the in vitro antimalarial potency superior to CQ.
► Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg × 4 days against CQ-resistant strain of P. yoelii.