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

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

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