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Polypharmacological drug actions of recently FDA approved antibiotics.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wetzel C,Lonneman M,Wu C

doi

10.1016/j.ejmech.2020.112931

subject

Has Abstract

pub_date

2021-01-01 00:00:00

pages

112931

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30903-X

journal_volume

209

pub_type

杂志文章,评审

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