Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
Novel artemisinin-quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90-110°C). All compounds were obtained as the β-isomers and were tested against both chloroquine sensitive and resistant strains of Plasmodium falciparum. Hybrid-dimer 8 showed the highest antiplasmodial activity, inheriting the optimum chain length of three carbon atoms.
Department of Pharmaceutical Chemistry, North-West University, Potchefstroom, South Africa.
Marli C
MC
Lombard
David D
DD
N'Da
Jaco C
JC
Breytenbach
Peter J
PJ
Smith
Carmen A
CA
Lategan
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry; D037621:Artemisinins / Q000737:chemistry* / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D019281:Dimerization; D004351:Drug Resistance; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology
D000962:Antimalarials; D037621:Artemisinins; D011804:Quinolines; D002738:Chloroquine