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Issue 1, 2016
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Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

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Abstract

Vast numbers of prevalent aminoglycoside-modifying enzymes undermine the clinical use of aminoglycoside antibiotics. We present the design and synthesis of a potent broad-spectrum bactericidal aminoglycoside based on available X-ray co-crystal structures within the ribosomal binding-site. The resulting antibiotic displays broad protection of its functional groups from inactivation by clinically relevant resistance enzymes.

Graphical abstract: Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

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Publication details

The article was received on 24 Sep 2015, accepted on 20 Oct 2015 and first published on 13 Nov 2015


Article type: Concise Article
DOI: 10.1039/C5MD00429B
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2016,7, 170-176
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    Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

    J. P. Maianti and S. Hanessian, Med. Chem. Commun., 2016, 7, 170
    DOI: 10.1039/C5MD00429B

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