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Issue 12, 2018
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Structure–activity relationship of the cinnamamide family of antibiotic potentiators for methicillin-resistant Staphylococcus aureus (MRSA)

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Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) is a global public health threat. MRSA has evolved a complex set of biochemical processes that mobilize the organism for inducible resistance on challenge by β-lactam antibiotics. Interfering pharmacologically with this machinery has the potential to reverse the β-lactam-resistance phenotype, whereby susceptibility to obsolete antibiotics would be restored. We describe herein our discovery of one class of such agents, the cinnamamide family of antibiotic potentiators. A hit compound of the class (compound 1) showed modest potentiation of the activity of oxacillin, a penicillin antibiotic, against an MRSA strain. A total of 50 analogues of compound 1 were prepared and screened. Seven of these compounds showed more dramatic potentiation of the antibacterial activity, which lowered the minimal-inhibitory concentrations (MICs) for the antibiotic by as much as 64- to 128-fold.

Graphical abstract: Structure–activity relationship of the cinnamamide family of antibiotic potentiators for methicillin-resistant Staphylococcus aureus (MRSA)

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Publication details

The article was received on 24 Sep 2018, accepted on 19 Oct 2018 and first published on 30 Oct 2018


Article type: Research Article
DOI: 10.1039/C8MD00479J
Citation: Med. Chem. Commun., 2018,9, 2008-2016

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    Structure–activity relationship of the cinnamamide family of antibiotic potentiators for methicillin-resistant Staphylococcus aureus (MRSA)

    E. Speri, J. Fishovitz and S. Mobashery, Med. Chem. Commun., 2018, 9, 2008
    DOI: 10.1039/C8MD00479J

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