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Branched Peptides: Acridine and Boronic Acid Derivatives as Antimicrobial Agents.

ABSTRACT: 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 ?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.

SUBMITTER: Wynn JE

PROVIDER: S-EPMC5554892 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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Branched Peptides: Acridine and Boronic Acid Derivatives as Antimicrobial Agents.

Wynn Jessica E JE Zhang Wenyu W Falkinham Joseph O JO Santos Webster L WL

ACS medicinal chemistry letters 20170712 8

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 μg/mL against Staphylococcus aureus, Candida albicans, and Escherichia coli. These peptides were nonhemolytic, and significantly inhibited growth of C. ...[more]

PMID: 28835795

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