Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2014 May 9;3(2):193-215.
doi: 10.3390/antibiotics3020193.

β-Lactam Antibiotics Renaissance

Wenling Qin  1 , Mauro Panunzio  2 , Stefano Biondi  3
Affiliations
Review

β-Lactam Antibiotics Renaissance

Wenling Qin et al. Antibiotics (Basel). .

Abstract

Since the 1940s β-lactam antibiotics have been used to treat bacterial infections. However, emergence and dissemination of β-lactam resistance has reached the point where many marketed β-lactams no longer are clinically effective. The increasing prevalence of multidrug-resistant bacteria and the progressive withdrawal of pharmaceutical companies from antibiotic research have evoked a strong reaction from health authorities, who have implemented initiatives to encourage the discovery of new antibacterials. Despite this gloomy scenario, several novel β-lactam antibiotics and β-lactamase inhibitors have recently progressed into clinical trials, and many more such compounds are being investigated. Here we seek to provide highlights of recent developments relating to the discovery of novel β-lactam antibiotics and β-lactamase inhibitors.

Keywords: bacterial infections; β-lactam antibiotics; β-lactamase inhibitors.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Chemical structure of CXA-101 and tazobactam.
Figure 2
Figure 2
Chemical structure of CAZ104 and avibactam.
Figure 3
Figure 3
Mechanism of action of avibactam.
Figure 4
Figure 4
Chemical structure of ceftaroline fosamil.
Figure 5
Figure 5
Chemical structures of imipenem, cilastatin, and MK-7655.
Figure 6
Figure 6
Reaction scheme for the improved synthesis of MK-7655.
Figure 7
Figure 7
Chemical structures of BAL30072.
Figure 8
Figure 8
Chemical structure of aztreonam.
Figure 9
Figure 9
Chemical structures of Carbavance.
Figure 10
Figure 10
Chemical structure of TD-1792.
Figure 11
Figure 11
Chemical structure of FPI-1465.
Figure 12
Figure 12
General structure of compounds claimed in WO2013/056079.
Figure 13
Figure 13
Synthesis of some sulfonamido boronic acids.
Figure 14
Figure 14
Chemical structure of arylboronic acids.
Figure 15
Figure 15
Chemical structure of arylboronic acids.
Figure 16
Figure 16
Chemical structure of diazabicyclooctane nitrile.
Figure 17
Figure 17
Chemical structure of antibacterial diazabicyclooctanes.
Figure 18
Figure 18
General structure of sulfonamido β-lactamase inhibitors.
Figure 19
Figure 19
Chemical synthesis of representative sulphonamido β-lactamase inhibitors.
Figure 20
Figure 20
Chemical structure of phosponate β-lactamase inhibitors.
Figure 21
Figure 21
Chemical structure of CB-027.
Figure 22
Figure 22
Chemical structure of FSI-1671.
See this image and copyright information in PMC

References

    1. Shlaes D.M. Antibiotics: The Perfect Storm. Springer Dordrec; Heilderberg, London, NY, USA: 2010.
    1. Pendleton J.N., Gorman S.P., Gilmore B.F. Clinical relevance of the eskape pathogens. Expert Rev. Anti-Infect. Ther. 2013;11:297–308. doi: 10.1586/eri.13.12. - DOI - PubMed
    1. Kallen A.J., Srinivasan A. Current epidemiology of multidrug-resistant gram-negative bacilli in the United States. Infect. Control. Hosp. Epidemiol. 2010;31:S51–S54. doi: 10.1086/655996. - DOI - PubMed
    1. Boucher H.W., Talbot G.H., Bradley J.S., Edwards J.E., Gilbert D., Rice L.B., Scheld M., Spellberg B., Bartlett J. Bad bugs, no drugs: No eskape! An update from the infectious diseases society of america. Clin. Infect. Dis. 2009;48:1–12. doi: 10.1086/595011. - DOI - PubMed
    1. Llarrull L.I., Testero S.A., Fisher J.F., Mobashery S. The future of the β-lactams. Curr. Opin. Microbiol. 2010;13:551–557. doi: 10.1016/j.mib.2010.09.008. - DOI - PMC - PubMed

LinkOut - more resources