Recent advances in the discovery of metallo-β-lactamase inhibitors for β-lactam antibiotic-resistant reversing agents.

Abstract:

:The overuse of antibiotics which exerts the selective pressure for bacterial pathogens has facilitated the spread of antibiotics' resistance. Metallo-β-lactamases (MβLs) are zinc enzymes produced by an increasing number of bacterial pathogens. They can readily cleave carbapenems and most other β-lactams that are mainstays of therapy for bacterial infections. MβL-conferred resistance to antibiotics is most worrisome due to MβLs exhibiting very broad-spectrum resistance. Therefore, the bacteria carrying MβLs have recently become a significant clinical threat. No clinically useful MβLs inhibitor has been discovered yet. To address the serious threat to public health posed by the MβL-conferred resistance to antibiotics, novel effective MβL inhibitors are urgently needed. This review mainly describes various MβL inhibitors, giving special attention to their antibacterial activity, mechanisms of action, structure-activity relationships and synergetic effect with clinically available antibiotics.

journal_name

Curr Drug Targets

journal_title

Current drug targets

authors

Guo Z,Ma S

doi

10.2174/1389450115666140326094504

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

689-702

issue

7

eissn

1389-4501

issn

1873-5592

pii

CDT-EPUB-59780

journal_volume

15

pub_type

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