Inhibition of bacterial resistance to aminoglycosides with novel prodrugs

Invention 10082

Inhibition of bacterial resistance to aminoglycosides with novel prodrugs

Novel prodrugs to inhibit the development of bacterial resistance to the important antibiotic aminoglycoside were developed at McGill University

Market Need

In a hospital setting, aminoglycosides are often used to treat serious infections as they are a broad-spectrum group of highly potent antibiotics. Similar to many other antibiotics, increased bacterial resistance to aminoglycoside has developed with continued use. Among the different bacterial mechanisms of resistance that have developed against aminoglycosides, one of the most clinically relevant is the expression of N-6’-acetyltransferase enzymes (AAC(6’)s).

Technology Summary

With this invention, the novel prodrug would be administered along with aminoglycosides to inhibit the spread of bacterial resistance to antibiotics in both Gram+ and Gram- bacteria. In particular, this compound is able to block the development of resistance to aminoglycosides by the enzyme AAC(6’)s. Along with an important inhibitory function, the drug also possesses a low cell cytotoxicity and good stability. Moreover, because of their activity against Gram-negative bacteria, the proposed drugs would fill one of the most important unmet needs in infectious disease treatments.

Advantages

• Prodrugs that inhibit bacterial resistance to the antibiotic aminoglycoside
• Also shows antibacterial resistance as a standalone drug

• Low cytotoxicity and molecularly stable

Patent Status

Issued US, EP