Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro.

Chitalu C Musonda; Susan Little; Vanessa Yardley; Kelly Chibale; (2007) Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro. Bioorganic & medicinal chemistry letters, 17 (17). pp. 4733-4736. ISSN 0960-894X DOI: 10.1016/j.bmcl.2007.06.070
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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.

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