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Quinoline‐based heterocyclic hydrazones: Design, synthesis, anti‐plasmodial assessment, and mechanistic insights.
- Source :
-
Chemical Biology & Drug Design . Apr2023, Vol. 101 Issue 4, p829-836. 8p. - Publication Year :
- 2023
-
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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *HYDRAZONES
*PLASMODIUM falciparum
*HYDRAZONE derivatives
*HEME
*QUINOLINE
Subjects
Details
- Language :
- English
- ISSN :
- 17470277
- Volume :
- 101
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- Chemical Biology & Drug Design
- Publication Type :
- Academic Journal
- Accession number :
- 162380456
- Full Text :
- https://doi.org/10.1111/cbdd.14185