Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: Synthesis and in vitro antimalarial evaluation

•Synthesis of urea and oxalamide tethered β-lactam-7-chloroquinoline conjugates.•Antimalarial evaluation against chloroquine-resistant W2 strain of Plasmodium falciparum.•Most potent of the tested compounds exhibited an IC50 of 34.97 nM.

The manuscript pertains to the synthesis of urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the β-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 of 34.97 nM against chloroquine resistant W2 strain of Plasmodium falciparum.

Graphical abstractSynthesis and in vitro antimalarial evaluation of urea and oxalamide tethered β-lactam-7-chloroquinoline conjugates.Figure optionsDownload full-size imageDownload as PowerPoint slide