Chemoselective Halogenation of Premarineosin A for Next-Generation Antimalarial Development

Authors

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.

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.

Preprint server: bioRxiv
The authors list and abstract were imported from bioRxiv on 18 Jun 2026.

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