One of the greatest threats to human health is the rise of antibiotic resistance in pathogenic bacteria, and failure of antibiotic treatment is becoming far more common. Aminoglycosides, a family of antibiotics, are far too often being rendered ineffective by bacterial aminoglycoside modifying enzymes. Of the various types of aminoglycoside modifying enzymes, the most common in clinical isolates is the AAC(6’)-Ib enzyme. In order to combat aminoglycoside modification by the AAC(6’)-Ib enzyme, previous work has screened potential small molecule inhibitors and identified a lead molecule inhibitor. We are working to synthesize and test the potency of this lead inhibitor on the AAC(6’)-Ib enzyme. Recently, the synthesis and purification of the lead inhibitor were optimized. Currently, work is underway to synthesize a library of derivatives of the lead inhibitor to also test on the AAC(6’)-Ib enzyme, which will aid in determining structure-activity relationships between the inhibitor and the AAC(6’)-Ib resistance enzyme.

Synthesis of potential AAC(6’)-Ib inhibitors to combat bacterial resistance to aminoglycoside antibiotics

253rd National Meeting (2017)

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