Antibiotic resistance is growing at an alarming rate, limiting the utility of current antibiotics. To address the antibiotic resistance crisis, our lab is investigating the use of antibiotic adjuvants to potentiate our arsenal of antibiotics. Antibiotic adjuvants are non-toxic compounds that disarm bacteria’s antibiotic resistance mechanisms, allowing antibiotics to be effective again. Our lab has identified two related scaffolds that potentiate β-lactam antibiotics in MRSA, namely brominated carbazoles and halogenated dibenzazepines. We sought to expand these scaffolds and develop structure-activity relationships and identify compounds with improved adjuvant activity. Several products have been synthesized and evaluated for biological activity. Synthetic methodologies, biological data, and a preliminary structure-activity relationship will be presented.

Synthesis and structural expansion of a novel antibiotic adjuvant scaffold to improve aqueous solubility and biological activity

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ACS Spring 2023

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