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Novel hybrid 1,4-naphthoquinone-endoperoxide antimalarial hits: synthesis, stereoisomeric separation, and biological evaluation
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DOI:10.1016/j.ejmech.2026.118926.png)
Abstract
En 中文
• First naphthoquinone-endoperoxide dual-pharmacophore antimalarial hybrids • Mn(III)-mediated peroxycyclization enabled access to stereoisomeric series • Full stereoisomer resolution was achieved by preparative chiral HPLC • Stereochemistry significantly influenced potency (3-fold) and selectivity (9-fold) • Lead exhibited IC50 0.49 μM against MDR P. falciparum W2 with SI >250 on CHO
Keywords:
naphthoquinone
endoperoxide
antimalarial
stereoisomers
hybrid compounds
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