Quinoline-based heterocyclic hydrazones: Design, synthesis, anti-plasmodial assessment, and mechanistic insights.

ABSTRACT

A library of quinoline-based hydrazones bearing 1H-1,2,3-triazole core was designed, synthesized, and evaluated for their antiplasmodial activity against the drug-resistant Plasmodium falciparum W2 strain. The inclusion of pyrazine-2-carboxylic acid with a flexible propyl spacer afforded the most active scaffold with an IC50 value of 0.26 µM. Mechanistically, the compound inhibited heme to hemozoin formation, as demonstrated by UV-vis and mass spectral studies.