ArticleOrganic & biomolecular chemistry2026
Chemoselective halogenation of premarineosin A for next-generation antimalarial development.
Article in Organic & biomolecular chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Premarineosin A undergoes rapid, chemoselective halogenation at C12 under mild conditions, enabling efficient access to brominated, chlorinated, fluorinated, and iodinated analogs without the need for protecting groups or extensive synthetic manipulation. Reaction conditions were optimized to favor selective functionalization of the electron-rich pyrrole ring while preserving the integrity of the macrocyclic scaffold. The resulting halogenated derivatives were readily isolated and characterized by LC-MS/MS and NMR spectroscopy. Biological evaluation revealed that all halogenated analogs retained potent antiplasmodial activity against both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2)
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