Apramycin, a unique broad spectrum aminoglycoside antibiotic, is only minimally susceptible to aminoglycoside modifying enzymes and has minimal ototoxicity compared to other aminoglycoside antibiotics. We have discovered that the O5 position can be modified without negatively affecting its interaction with the binding pocket in the decoding A site on helix 44 of the rRNA. In this poster we describe strategies for the derivatization at the O5 position of apramycin and present the subsequent structure-activity relationships resulting in significantly improved apramycin derivatives

Design, synthesis, and evaluation of O5 modified apramycin derivatives

2019 Fall National Meeting

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