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Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant an...

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Detalles Bibliográficos
Autor principal: Konaklieva, Monika I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4790389/
https://www.ncbi.nlm.nih.gov/pubmed/27025739
http://dx.doi.org/10.3390/antibiotics3020128
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author Konaklieva, Monika I.
author_facet Konaklieva, Monika I.
author_sort Konaklieva, Monika I.
collection PubMed
description The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets.
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spelling pubmed-47903892016-03-24 Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects Konaklieva, Monika I. Antibiotics (Basel) Review The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets. MDPI 2014-04-03 /pmc/articles/PMC4790389/ /pubmed/27025739 http://dx.doi.org/10.3390/antibiotics3020128 Text en © 2014 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Konaklieva, Monika I.
Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title_full Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title_fullStr Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title_full_unstemmed Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title_short Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
title_sort molecular targets of β-lactam-based antimicrobials: beyond the usual suspects
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4790389/
https://www.ncbi.nlm.nih.gov/pubmed/27025739
http://dx.doi.org/10.3390/antibiotics3020128
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