Aminoglycosides Scaffolding Targeting Antibiotic-Resistant Bacteria

Summary This invention encompasses key modifications to the chemistry of aminoglycosides to overcome bacterial resistance. The novel chemistry leverages: (a) the weak stereospecificity of aminoglycoside binding to rRNA, and (b) the stereospecific binding of extrinsic enzymes shown to inactivate aminoglycosides. These distinct properties are used to generate aminoglycoside enantiomers and diastereomers able to escape enzyme-mediated resistance and also reduce future resistance generation. Experiments used modified neamine, whereby L-neamine was also found to inhibit the in-vitro translation of E. coli and P. aeruginosa similar to D-neamine. Most importantly, L-neamine was able to inhibit growth of aminoglycoside-resistant E. coli, suggesting a new therapeutic avenue against enzyme-mediated antibiotic resistance.

Applications Aminoglycoside analogs may serve as broad-spectrum antibiotics effective against enterococcal, mycobacterial, and gram-negative infections, including E. coli, Pseudomonas, and certain antibiotic-resistant strains of bacteria. For Further Information Please Contact the Director of Business Development Michal Preminger Email: michal_preminger@hms.harvard.edu Telephone: (617) 432-0920

Inventor(s): Rando, Robert R

Type of Offer: Licensing



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