| 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 |