4.5 Article

Branched Peptides: Acridine and Boronic Acid Derivatives as Antimicrobial Agents

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 8, Issue 8, Pages 820-823

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00119

Keywords

Branched peptides; Acridine; Boronic Acid; MIC; Antimicrobials; Biofilms

Funding

  1. NIH Grant [R01 GM093834]

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The emergence of microbial resistance presents a challenge in the development of next generation therapeutics. Herein, we report the discovery of branched peptides decorated with acridine and boronic acid moieties with potent antimicrobial activity. The results revealed minimal inhibitory concentrations (MICs) as low as 1 mu g/mL against Staphylococcus aureus, Candida albicans, and Escherichia coli. These peptides were nonhemolytic, and significantly inhibited growth of C. albicans in suspension and biofilm formation. Structure-activity relationship studies suggest the acridine functional group as a driving force for the potent inhibition observed against bacteria.

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