Evaluation of 4-Aminoquinoline Hydrazone Analogues as Potential Leads for Drug-Resistant Malaria.

ABSTRACT: The emergence of resistance to first-line antimalarial drugs calls for the development of new therapies for drug-resistant malaria. The efficacy of quinoline-based antimalarial drugs has prompted the development of novel quinolines. A panel of 4-aminoquinoline hydrazone analogues were tested on the multidrug-resistant K1 strain of Plasmodium falciparum: IC₅₀ values after a 48 h cycle ranged from 0.60 to 49 µM, while the 72 h cycle ranged from 0.026 to 0.219 μM. Time-course assays were carried out to define the activity of the lead compounds, which inhibited over 50% growth in 24 h and 90% growth in 72 h. Cytotoxicity assays with HepG2 cells showed IC₅₀ values of 0.87-11.1 μM, whereas in MDBK cells, IC₅₀ values ranged from 1.66 to 11.7 μM. High select

SUBMITTER: Magwaza RN 

PROVIDER: S-EPMC10534891 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature