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dc.contributor.authorBreytenbach, Jaco Cornelius
dc.contributor.authorLombard, Martha Carolina
dc.contributor.authorN'da, David Dago
dc.contributor.authorLategan, Carmen A.
dc.contributor.authorSmith, Peter J.
dc.date.accessioned2012-09-11T11:31:24Z
dc.date.available2012-09-11T11:31:24Z
dc.date.issued2011
dc.identifier.citationLombard, 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.issn0960-894X
dc.identifier.issn1464-3405 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/7384
dc.description.abstractDihydroartemisinin (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.urihttp://dx.doi.org/10.1016/j.bmcl.2011.01.103
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectArtemisininen_US
dc.subjectmalariaen_US
dc.subjecthybridsen_US
dc.subjectquinolineen_US
dc.titleSynthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybridsen_US
dc.typeArticleen_US


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