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July 18, 2014

VIP: Importance of the 6'-Hydroxy Group and Its Configuration for Apramycin Activity

VIP: Importance of the 6'-Hydroxy Group and Its Configuration for Apramycin ActivityAppi Reddy Mandhapati, Dimitri Shcherbakov, Stefan Duscha, Andrea Vasella,* Erik C. Böttger,* David Crich*

The relative lack of success of combinatorial drug discovery platforms in the search for novel antibacterial drugs warrants a renewed focus on the optimization of established drug classes such as the aminoglycoside antibiotics. Most aminoglycosides in current use suffer from toxicity problems, the most serious of which is drug-induced ototoxicity.

Researchers in this collaboration focus on apramycin, an aminoglycoside antibiotic currently only used in veterinary medicine, that has previously been demonstrated to be substantially ototoxicity-free and efficacious in the treatment of methicillin-resistant Staphylococcus aureus in animal models. Read more...

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    Dr. Richard J. Fair, Dr. Lisa S. McCoy, Dr. Mary E. Hensler, Bernice Aguilar, Prof. Dr. Victor Nizet and Prof. Dr. Yitzhak Tor

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    Irresistible! Amikacin and tobramycin are two clinically useful RNA-targeting aminoglycosides. Modified versions of these compounds showed equal to or better potency against certain resistant bacterial strains, while their eukaryotic cytotoxicity remained identical to that of the parent antibiotics.

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