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Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids

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dc.contributor.author Breytenbach, Jaco Cornelius
dc.contributor.author Lombard, Martha Carolina
dc.contributor.author N'da, David Dago
dc.contributor.author Lategan, Carmen A.
dc.contributor.author Smith, Peter J.
dc.date.accessioned 2012-09-11T11:31:24Z
dc.date.available 2012-09-11T11:31:24Z
dc.date.issued 2011
dc.identifier.citation Lombard, M.C. et al. 2011. Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids. Bioorganic & medicinal chemistry letters, 21(6):1683-1686. [http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry-letters/] en_US
dc.identifier.issn 0960-894X
dc.identifier.issn 1464-3405 (Online)
dc.identifier.uri http://hdl.handle.net/10394/7384
dc.description.abstract Dihydroartemisinin (DHA) was coupled to different aminoquinoline moieties forming hybrids 9–14, which were then treated with oxalic acid to form oxalate salts (9a–14a). Compounds 9a, 10a, 12, 12a, and 14a showed comparable potency in vitro to that of chloroquine (CQ) against the chloroquine sensitive (CQS) strain, and were found to be more potent against the chloroquine resistant CQR strain. Hybrids 12 and its oxalate salt 12a were the most active against CQR strain, being 9- and 7-fold more active than CQ, respectively (17.12 nM; 20.76 nM vs 157.9 nM). An optimum chain length was identified having 2 or 3 Cs with or without an extra methylene substituent. en_US
dc.description.uri http://dx.doi.org/10.1016/j.bmcl.2011.01.103
dc.language.iso en en_US
dc.publisher Elsevier en_US
dc.subject Artemisinin en_US
dc.subject malaria en_US
dc.subject hybrids en_US
dc.subject quinoline en_US
dc.title Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids en_US
dc.type Article en_US


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