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Chemoselective Halogenation of Premarineosin A for Next-Generation Antimalarial Development

Harris, N. R.; Amin, S.; Curtis, B. J.; Teklemichael, A. A.; Dranchak, P.; McBride, C. M.; Verhey-Henke, L.; Warrell, C. J.; Dulaney, W. M.; Oliphant, E. N.; Inglese, J.; Su, X.-z.; Sherman, D. H.; Pereira, F.

2026-06-17 biochemistry
10.64898/2026.06.16.732709 bioRxiv
Show abstract

Premarineosin A undergoes rapid, chemoselective C12 halogenation under mild conditions, providing brominated, chlorinated, fluorinated, and iodinated analogs. These derivatives retained potent antiplasmodial activity against both chloroquine-sensitive and -resistant Plasmodium falciparum strains and displayed smaller reductions in potency against the resistant strain than the parent compound.

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