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bioRxiv · 10.64898/2026.06.16.732709

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.
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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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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. Chemoselective Halogenation of Premarineosin A for Next-Generation Antimalarial Development. https://doi.org/10.64898/2026.06.16.732709

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