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Review
. 2021 Jan 1:209:112931.
doi: 10.1016/j.ejmech.2020.112931. Epub 2020 Oct 14.

Polypharmacological drug actions of recently FDA approved antibiotics

Carlie Wetzel  1 , Mitchell Lonneman  1 , Chun Wu  2
Affiliations
Review

Polypharmacological drug actions of recently FDA approved antibiotics

Carlie Wetzel et al. Eur J Med Chem. .

Abstract

The current epidemic of antibiotic resistant bacterial infections has fueled the demand for novel antibiotics exhibiting both antibacterial efficacy and anti-drug resistance. This need has not been fully satisfied by the conventional "one target-one molecule" approach. Consequently, there has been rising interest in the development of multi-target antibiotics. Over the past two decades, 52% (14 out of 27) of the FDA approved antibiotics have demonstrated synergistic, multi-target mechanisms of action. Among these are three second-generation lipoglycopeptides, five new generation quinolones and six modernized β-lactams. This review focuses on the structure-activity relationship (SAR) analysis and the polypharmacological drug action of these antibiotics, to reveal how these multi-target antibiotics achieve the dual objectives of maximizing bactericidal or bacteriostatic efficacy and minimizing antibiotic resistance. The entrance of multi-target antibiotics into the FDA-approved regimens represents a milestone in the evolution of drug discovery as it has transcended from chemical library screening to rational drug design.

Keywords: Antibiotics 3; Drug resistance 4; Multi-target 2; Polypharmacology 1.

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Conflict of interest statement

Declaration of competing interest I confirm that the manuscript has been submitted solely to “European Journal of Medicinal Chemistry” Journal and is not published, in the press, or submitted elsewhere and there is no conflict of interest.

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