Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity

Frequency of malaria and its resistance to chemotherapeutic options are emerging rapidly. To counter this problem, a series of 4-aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized and screened for their antimalarial activities. Triazine derivative 48 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro assay with an IC50 of 5.23 ng/mL and oxalamide derivative 13 showed an in vivo suppression of 70.45% on day 4 against CQ resistant strain N-67 of Plasmodiumyoelii.

In search of novel 4-aminoquinolines to counteract the problem of resistance, side chain incorporated oxalamide and triazine derivatives were synthesized and screened for their antimalarial activities. Compounds 48, 41 showed potent activity of IC50 5.23, 7.88 ng/mL, respectively and compound 12 showed above moderate activity of IC50 15.58 ng/mL against 3D7 strain of Plasmodium falciparum.Figure optionsDownload as PowerPoint slide