Aminoglycosides are a class of antibiotics that are used primarily to treat Gram-negative infections, as well as some Gram-positive and Mycobacterium infections.  High-level resistance is conferred by the actions of aminoglycoside-modifying enzymes such as aminoglycoside N-acetyltransferases (AACs), aminoglycoside nucleotidyltransferases (ANTs), and aminoglycoside phosphtransferases (APHs).  It is therefore hypothesized that if these enzymes are inhibited, that resistance will be lost, and bacteria will once again be susceptible to these antimicrobials.<br/>Preliminary screening identified three leads with inhibitory activity against ANT (2”)-Ia and/or AAC(3)-Ia.  Parallel synthetic strategies were developed to build chemical libraries around these scaffolds (containing biphenyl, oxindole, and quinazoline cores), and the compounds were assayed against their respective targets.  Results will be discussed.<br/>

Development of aminoglycoside resistance enzyme inhibitors as a means to rescue antibiotic activity

256th National Meeting (2018)

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