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.

Graphical abstractThe synthesis and biological activity of a new series of 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles is described.Figure optionsDownload full-size imageDownload as PowerPoint slide