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Synthesis and in vitro antiplasmodial activity of quinoline-ferrocene esters

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dc.contributor.author Breytenbach, Jaco Cornelius
dc.contributor.author Lategan, Carmen
dc.contributor.author N'da, David Dago
dc.contributor.author Smith, Peter J.
dc.date.accessioned 2012-09-03T09:32:38Z
dc.date.available 2012-09-03T09:32:38Z
dc.date.issued 2011
dc.identifier.citation N'da, D.D. et al. 2011. Synthesis and in vitro antiplasmodial activity of quinoline-ferrocene esters. Arzneimittelforschung: drug research, 61(6):358-365. [http://www.thieme.com/index.php?page=shop.product_details&flypage=flypage.tpl&product_id=1380&category_id=2&keyword=Arzneimittelforschung&option=com_virtuem] en_US
dc.identifier.issn 0004-4172
dc.identifier.uri http://hdl.handle.net/10394/7200
dc.description.abstract New 4-aminoquinoline-derived esters containing the redox-active ferrocene group brought in by either ferrocenyformic or 4-ferrocenylbutanoic acids were synthesized and tested in vitro for their antiplasmodial activity. The results revealed that only esters derived from ferrocenylformic acid were active against both chloroquine (CQ)-resistant Dd2 and CQ-sensitive D10 strains of Plasmodium falciparum. However, none of these showed higher actvity than CQ against the sensitive strain. Ester 16, which possesses a butyl branch in the structure, was the most active of all. With an IC50 of 0.13 mM on the resistant strain, this ester possessed 2.5-fold higher activity than CQ (IC50 = 0.34 mM). All tested esters showed good selectivity towards P. falciparum with indexes higher than 60. en_US
dc.language.iso en en_US
dc.publisher Thieme publishing en_US
dc.title Synthesis and in vitro antiplasmodial activity of quinoline-ferrocene esters en_US
dc.type Article en_US


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