The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis

We identified a series of novel 7-phenyl benzoxaborole compounds with activity against Mycobacterium tuberculosis. Compounds had a range of activity with inhibitory concentrations (IC(90)) as low as 5.1 μM and no cytotoxicity against eukaryotic cells (IC(50) > 50 μM). Compounds were active agains...

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Autores principales: Korkegian, Aaron, O'Malley, Theresa, Xia, Yi, Zhou, Yasheen, Carter, David S., Sunde, Bjorn, Flint, Lindsay, Thompson, Dean, Ioerger, Thomas R., Sacchettini, Jim, Alley, M.R.K., Parish, Tanya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Churchill Livingstone 2018
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5854369/
https://www.ncbi.nlm.nih.gov/pubmed/29523334
http://dx.doi.org/10.1016/j.tube.2017.11.003
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author Korkegian, Aaron
O'Malley, Theresa
Xia, Yi
Zhou, Yasheen
Carter, David S.
Sunde, Bjorn
Flint, Lindsay
Thompson, Dean
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M.R.K.
Parish, Tanya
author_facet Korkegian, Aaron
O'Malley, Theresa
Xia, Yi
Zhou, Yasheen
Carter, David S.
Sunde, Bjorn
Flint, Lindsay
Thompson, Dean
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M.R.K.
Parish, Tanya
author_sort Korkegian, Aaron
collection PubMed
description We identified a series of novel 7-phenyl benzoxaborole compounds with activity against Mycobacterium tuberculosis. Compounds had a range of activity with inhibitory concentrations (IC(90)) as low as 5.1 μM and no cytotoxicity against eukaryotic cells (IC(50) > 50 μM). Compounds were active against intracellular mycobacteria cultured in THP-1 macrophages. We isolated and characterized resistant mutants with mutations in NADH dehydrogenase (Ndh) or the regulatory protein Mce3R. Mutations suggest that Ndh may be the target of this series.
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spelling pubmed-58543692018-03-16 The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis Korkegian, Aaron O'Malley, Theresa Xia, Yi Zhou, Yasheen Carter, David S. Sunde, Bjorn Flint, Lindsay Thompson, Dean Ioerger, Thomas R. Sacchettini, Jim Alley, M.R.K. Parish, Tanya Tuberculosis (Edinb) Article We identified a series of novel 7-phenyl benzoxaborole compounds with activity against Mycobacterium tuberculosis. Compounds had a range of activity with inhibitory concentrations (IC(90)) as low as 5.1 μM and no cytotoxicity against eukaryotic cells (IC(50) > 50 μM). Compounds were active against intracellular mycobacteria cultured in THP-1 macrophages. We isolated and characterized resistant mutants with mutations in NADH dehydrogenase (Ndh) or the regulatory protein Mce3R. Mutations suggest that Ndh may be the target of this series. Churchill Livingstone 2018-01 /pmc/articles/PMC5854369/ /pubmed/29523334 http://dx.doi.org/10.1016/j.tube.2017.11.003 Text en © 2017 The Authors http://creativecommons.org/licenses/by/4.0/ This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Korkegian, Aaron
O'Malley, Theresa
Xia, Yi
Zhou, Yasheen
Carter, David S.
Sunde, Bjorn
Flint, Lindsay
Thompson, Dean
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M.R.K.
Parish, Tanya
The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title_full The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title_fullStr The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title_full_unstemmed The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title_short The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
title_sort 7-phenyl benzoxaborole series is active against mycobacterium tuberculosis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5854369/
https://www.ncbi.nlm.nih.gov/pubmed/29523334
http://dx.doi.org/10.1016/j.tube.2017.11.003
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