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Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)‑N‑Benzoyl-3-phenylisoserine
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https://doi.org/10.1021/ml400164tAbstract
A series of hybrid compounds based on (2R,3S)-N-benzoyl-3-phenylisoserine, artemisinin, and quinoline moieties was synthesized and tested for in vitro antiplasmodial activity against erythrocytic stages of K1 and W2 strains of Plasmodium falciparum. Two hybrid compounds incorporating (2R,3S)-N-benzoyl-3-phenylisoserine and artemisinin scaffolds were 3- to 4-fold more active than dihydroartemisinin, with nanomolar IC50 values against Plasmodium falciparum K1 strain.
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