4-Aminoquinoline quinolizidinyl- and quinolizidinylalkyl-derivatives with antimalarial activity.
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.
Sparatore
Anna
A
Institute of Medicinal Chemistry, University of Milan, Viale Abruzzi, 42, 20131 Milan, Italy. anna.sparatore@unimi.it
Basilico
Nicoletta
N
Parapini
Silvia
S
Romeo
Sergio
S
Novelli
Federica
F
Sparatore
Fabio
F
Taramelli
Donatella
D
D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D002738:Chloroquine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects*; D010967:Plasmodium yoelii / Q000187:drug effects; D011807:Quinolizines / Q000138:chemical synthesis / Q000494:pharmacology*
D000634:Aminoquinolines; D000962:Antimalarials; D011807:Quinolizines; D002738:Chloroquine; C001920:4-aminoquinoline