Abstract
Tetraoxaquines, molecular hybrids of 1,2,4,5-tetraoxane and 4-aminoquinoline, were designed via molecular docking analysis against Falcipain-2. Among the studied compounds, 11 top scoring analogues showing low binding energy were further selected for synthesis and evaluated for their in vitro antimalarial activity. In inhibitory assay, five compounds showed significant activity against chloroquine-resistant strain of P. falciparum-RKL-9 with IC50 values of 3.906, 3.942, 4.272, 3.906, 4.814 µg/ml.
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