A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro

We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis. The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentra...

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Autores principales: Patel, Nipul, O'Malley, Theresa, Zhang, Yong-Kang, Xia, Yi, Sunde, Bjorn, Flint, Lindsay, Korkegian, Aaron, Ioerger, Thomas R., Sacchettini, Jim, Alley, M. R. K., Parish, Tanya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Society for Microbiology 2017
Materias:
Mechanisms of Resistance
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571309/
https://www.ncbi.nlm.nih.gov/pubmed/28674058
http://dx.doi.org/10.1128/AAC.01205-17
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author Patel, Nipul
O'Malley, Theresa
Zhang, Yong-Kang
Xia, Yi
Sunde, Bjorn
Flint, Lindsay
Korkegian, Aaron
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M. R. K.
Parish, Tanya
author_facet Patel, Nipul
O'Malley, Theresa
Zhang, Yong-Kang
Xia, Yi
Sunde, Bjorn
Flint, Lindsay
Korkegian, Aaron
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M. R. K.
Parish, Tanya
author_sort Patel, Nipul
collection PubMed
description We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis. The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentration [IC(50)] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC(50) > 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.
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spelling pubmed-55713092017-09-05 A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro Patel, Nipul O'Malley, Theresa Zhang, Yong-Kang Xia, Yi Sunde, Bjorn Flint, Lindsay Korkegian, Aaron Ioerger, Thomas R. Sacchettini, Jim Alley, M. R. K. Parish, Tanya Antimicrob Agents Chemother Mechanisms of Resistance We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis. The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentration [IC(50)] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC(50) > 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c. American Society for Microbiology 2017-08-24 /pmc/articles/PMC5571309/ /pubmed/28674058 http://dx.doi.org/10.1128/AAC.01205-17 Text en Copyright © 2017 Patel et al. https://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Mechanisms of Resistance
Patel, Nipul
O'Malley, Theresa
Zhang, Yong-Kang
Xia, Yi
Sunde, Bjorn
Flint, Lindsay
Korkegian, Aaron
Ioerger, Thomas R.
Sacchettini, Jim
Alley, M. R. K.
Parish, Tanya
A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title_full A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title_fullStr A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title_full_unstemmed A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title_short A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro
title_sort novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro
topic Mechanisms of Resistance
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571309/
https://www.ncbi.nlm.nih.gov/pubmed/28674058
http://dx.doi.org/10.1128/AAC.01205-17
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