Synthesis, characterization and antimalarial activity of quinoline-pyrimidine hybrids
Date
2013Author
Pretorius, Stefan I.
Breytenbach, Wilma J.
N'Da, David D.
De Kock, Carmen
Smith, Peter J.
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The aim of this study was to synthesize a series of quinoline–pyrimidine hybrids and to evaluate their
in vitro antimalarial activity as well as cytotoxicity. The hybrids were brought about in a two-step nucleophilic
substitution process involving quinoline and pyrimidine moieties. They were screened alongside
chloroquine (CQ), pyrimethamine (PM) and fixed combinations thereof against the D10 and Dd2 strains
of Plasmodium falciparum. The cytotoxicity was determined against the mammalian Chinese Hamster
Ovarian cell line. The compounds were all active against both strains. However, hybrid (21) featuring
piperazine linker stood as the most active of all. It was found as potent as CQ and PM against the D10
strain, and possessed a moderately superior potency over CQ against the Dd2 strain (IC50: 0.157 vs
0.417 lM, threefold), and also displayed activity comparable to that of the equimolar fixed combination
of CQ and PM against both strains
URI
http://hdl.handle.net/10394/17526https://www.sciencedirect.com/science/article/pii/S0968089612008346
https://doi.org/10.1016/j.bmc.2012.10.019