N, N-Bis (trifluoromethylquinoline-4-yl)diamino alkanes: synthesis and antimalarial activity
Date
2008Author
Kgokong, J.L.
Matsabisa, G.M.
Smith, P.P.
Breytenbach, Jaco C.
Metadata
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A series of N,N-bis(trifluoromethylquinolin-4-yl)- and N,N-bis[2,8-bis(trifluoromethyl)quinolin-4-yl] diamino alkane and piperazine derivatives were synthesised by employing a simple and rapid displacement reaction of the 4-chloro group on the 2-trifluoromethyl- and 2,8-bis(trifluoromethyl)-quinoline by diaminoalkane or piperazine groups. Results of in vitro antimalarial activity evaluations of these compounds against the chloroquine-sensitive (D10) and chloroquineresistant (K1) strains of Plasmodium falciparum indicate that compounds with trifluoromethyl groups in both the 2 and 8 positions coupled with diaminoalkyl bridging chains of 2 to 6 carbon atoms exhibit a slightly higher activity than compound with only a trifluoromethyl group at position 2, and those with a piperazine bridge These compounds exhibit higher activity in the chloroquine-resistant than in the chloroquine-sensitive strains of the Plasmodium. Comparative studies indicate that the compounds are more selective in their cytotoxicity against the parasite cells. Except for compounds containing a piperazine bridge, this new series of compounds interact with ferriprotoporphyrin IX to more or less the same extent
URI
http://hdl.handle.net/10394/3078https://www.eurekaselect.com/83145/article/nn-bistrifluoromethylquinolin-4-yldiamino-alkanes-synthesis-and-antimalarial-activity
https://doi.org/10.2174/157340608785700216
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- Faculty of Health Sciences [2386]