A novel artemisinin-quinine hybrid with potent antimalarial activity.
Artemisinin was reduced to dihydroartemisinin and coupled to a carboxylic acid derivative of quinine via an ester linkage. This novel hybrid molecule had potent activity against the 3D7 and (drug-resistant) FcB1 strains of Plasmodium falciparum in culture. The activity was superior to that of artemisinin alone, quinine alone, or a 1:1 mixture of artemisinin and quinine.
Walsh
John J
JJ
School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, Dublin 2, Ireland. jjwalsh@tcd.ie <jjwalsh@tcd.ie>
Coughlan
David
D
Heneghan
Nicola
N
Gaynor
Caroline
C
Bell
Angus
A
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum; D011803:Quinine / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors
D000962:Antimalarials; D037621:Artemisinins; C031327:artemisinin; D011803:Quinine