Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro.
The synthesis and antimalarial activity of a novel series of first generation 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles against two strains of the Plasmodium falciparum parasite in vitro is described. A number of compounds significantly more potent than the standard drug chloroquine were identified.
Musonda
Chitalu C
CC
Department of Chemistry, University of Cape Town, Rondebosch, South Africa.
Little
Susan
S
Yardley
Vanessa
V
Chibale
Kelly
K
D000634:Aminoquinolines / Q000737:chemistry*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D010080:Oxazoles / Q000737:chemistry*; D021261:Parasitic Sensitivity Tests; D010961:Plasmodium / Q000378:metabolism; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000962:Antimalarials; D010080:Oxazoles; C001920:4-aminoquinoline