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Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective

[Image: see text] The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but also provide at least inte...

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Autores principales: Kolarič, Anja, Anderluh, Marko, Minovski, Nikola
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7307926/
https://www.ncbi.nlm.nih.gov/pubmed/32027491
http://dx.doi.org/10.1021/acs.jmedchem.9b01738
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author Kolarič, Anja
Anderluh, Marko
Minovski, Nikola
author_facet Kolarič, Anja
Anderluh, Marko
Minovski, Nikola
author_sort Kolarič, Anja
collection PubMed
description [Image: see text] The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but also provide at least interim effective protection against emerging bacterial infections. Research into DNA gyrase and topoisomerase IV inhibitors has become a particular focus, with the description of a new class of bacterial topoisomerase type II inhibitors known as “novel bacterial topoisomerase inhibitors”, NBTIs. Elucidation of the key structural modifications incorporated into these inhibitors and the impact these can have on their general physicochemical properties are detailed in this review. This defines novel bacterial topoisomerase inhibitors with promising antibacterial activities and potencies, which thus represent one potential example of the future “drugs for bad bugs”, as identified by the World Health Organization.
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spelling pubmed-73079262020-06-23 Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective Kolarič, Anja Anderluh, Marko Minovski, Nikola J Med Chem [Image: see text] The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but also provide at least interim effective protection against emerging bacterial infections. Research into DNA gyrase and topoisomerase IV inhibitors has become a particular focus, with the description of a new class of bacterial topoisomerase type II inhibitors known as “novel bacterial topoisomerase inhibitors”, NBTIs. Elucidation of the key structural modifications incorporated into these inhibitors and the impact these can have on their general physicochemical properties are detailed in this review. This defines novel bacterial topoisomerase inhibitors with promising antibacterial activities and potencies, which thus represent one potential example of the future “drugs for bad bugs”, as identified by the World Health Organization. American Chemical Society 2020-02-06 2020-06-11 /pmc/articles/PMC7307926/ /pubmed/32027491 http://dx.doi.org/10.1021/acs.jmedchem.9b01738 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Kolarič, Anja
Anderluh, Marko
Minovski, Nikola
Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title_full Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title_fullStr Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title_full_unstemmed Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title_short Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs): Miniperspective
title_sort two decades of successful sar-grounded stories of the novel bacterial topoisomerase inhibitors (nbtis): miniperspective
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7307926/
https://www.ncbi.nlm.nih.gov/pubmed/32027491
http://dx.doi.org/10.1021/acs.jmedchem.9b01738
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