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

Bharvi Sharma, Shefali Chowdhary, Jenny Legac, Philip J. Rosenthal, Vipan Kumar

Chemical Biology & Drug Design · 2022 · 10 citations · 21 references

Concepts

Abstract

Abstract A library of quinoline‐based hydrazones bearing 1 H ‐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 IC 50 value of 0.26 μM. Mechanistically, the compound inhibited heme to hemozoin formation, as demonstrated by UV–vis and mass spectral studies.

References

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