Antimalarial activity of 10-alkyl/aryl esters and – aminoethylethers of artemisinin
Date
2013Author
Cloete, Theunis T.
N’Da, David D.
Krebs, Henk J.
Clark, Julie A.
Connelly, Michele C.
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Show full item recordAbstract
A series of n-alkyl/aryl esters were synthesized and their in vitro antiplasmodial activity was measured
alongside that of previously synthesized aminoethylethers of artemisinin ozonides against various strains
of Plasmodium falciparum. The cytotoxicity against human cell lines was also assessed. The esters were
synthesized in a one-step reaction by derivatization on carbon C-10 of dihydroartemisinin. Both classes
were active against both the 3D7 and K1 strains of P. falciparum, with all compounds being significantly
more potent than artemether against both strains. The majority of compounds possessed potency either
comparable or more than artesunate with a high degree of selectivity towards the parasitic cells. The
10a-n-propyl 11 and 10a-benzyl 18 esters were the most potent of all synthesized ozonides, possessing
a moderate ( 3-fold) and significant (22- and 12-fold, respectively) potency increases against the 3D7
and K1 strains, respectively, in comparison with artesunate.
URI
http://hdl.handle.net/10394/13694https://www.sciencedirect.com/science/article/pii/S004520681200048X
https://doi.org/10.1016/j.bioorg.2012.10.002
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- Faculty of Health Sciences [2386]