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Structure-Activity Relationship of the Cinnamamide Family of Antibiotic Potentiators for Methicillin-Resistance Staphylococcus aureus (MRSA)

Abstract

Methicillin-Resistant Staphylococcus aureus (MRSA) is a global public health threat. MRSA has evolved a complex set of biochemical processes that mobilizes the organism for inducible resistance on challenge by β-lactam antibiotics. To interfere 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 a modest potentiation of the activitiy 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 a 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.

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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, Accepted Manuscript
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    Structure-Activity Relationship of the Cinnamamide Family of Antibiotic Potentiators for Methicillin-Resistance Staphylococcus aureus (MRSA)

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

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