Chemoselective Halogenation of Premarineosin A for Next-Generation Antimalarial Development
Natalia R. HarrisiD, Sahar Amin, Brian J. CurtisiD, Awet Alem TeklemichaeliD, Patricia K. DranchakiD, Christina M. McBrideiD, Linnea Verhey-Henke, Chloe J. Warrell, William M. Dulaney, Erin N. OliphantiD, James IngleseiD, Xin‐zhuan SuiD, David H. ShermaniD, Filipa M. PereiraiD
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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