A set of quinolizidinyl and quinolizidinylalkyl derivatives of 4-amino-7-chloroquinoline and of 9-amino-6-chloro-2-methoxyacridine were prepared and tested in vitro against CQ-sensitive (D-10) and CQ-resistant (W-2) strains of Plasmodium falciparum. All compounds but one exerted significant antimalarial activity. Some of the quinolizidine derivatives were from 5 to 10 times more active than chloroquine on the CQ-resistant strain. No toxicity against mammalian cells was observed.
4-Aminoquinoline quinolizidinyl- and quinolizidinylalkyl-derivatives with antimalarial activity
NOVELLI, FEDERICA;SPARATORE, FABIO;
2005-01-01
Abstract
A set of quinolizidinyl and quinolizidinylalkyl derivatives of 4-amino-7-chloroquinoline and of 9-amino-6-chloro-2-methoxyacridine were prepared and tested in vitro against CQ-sensitive (D-10) and CQ-resistant (W-2) strains of Plasmodium falciparum. All compounds but one exerted significant antimalarial activity. Some of the quinolizidine derivatives were from 5 to 10 times more active than chloroquine on the CQ-resistant strain. No toxicity against mammalian cells was observed.
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