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The site‐selective modification of complex biomolecules by transition metal‐catalysis is highly warranted, but often thwarted by the presence of Lewis basic functional groups. This study demonstrates that protonation of amines and phosphates in carbohydrates circumvents catalyst inhibition in palladium‐catalyzed site‐selective oxidation. Both aminoglycosides and sugar phosphates, compound classes...
We report the synthesis and evaluation of two new apramycin 5‐O‐β‐d‐ribofuranosides, or apralogs, carrying aminoalkyl branches at the ribofuranose 4‐position. This novel modification conveys excellent activity for the inhibition of protein synthesis by wild‐type bacterial ribosomes and correspondingly high antibacterial activity against several Gram‐negative pathogens. Notably, these new modifications...
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