Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents

The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened against CQ sensitive strain 3D7 of P. falciparum in an in vitro model. Compounds 65 and 69 exhibited more than 99% suppression on day 4 and on day 6 post treatment, compound 69 showed impressive 99.11% suppression against CQ resistant strain N-67 of P. yoelii in an in vivo assay.

Graphical abstractA series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened against CQ sensitive strain 3D7 of P. falciparum in an in vitro model and CQ resistant strain N-67 of P. yoelii in an in vivo assay. The compounds 65 and 69 exhibited more than 99% suppression on day 4.Figure optionsDownload full-size imageDownload as PowerPoint slide