A novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro

Nipul Patel; Theresa O’Malley; Yong Kang Zhang; Yi Xia; Bjorn Sunde; Lindsay Flint; Aaron Korkegian; Thomas R. Ioerger; Jim Sacchettini; M. R.K. Alley; Tanya Parish

doi:10.1128/AAC.01205-17

A novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro

Nipul Patel
, Theresa O’Malley
, Yong Kang Zhang
, Yi Xia
, Bjorn Sunde
, Lindsay Flint
, Aaron Korkegian
, Thomas R. Ioerger
, Jim Sacchettini
, M. R.K. Alley
, Tanya Parish

Infectious Disease Research Institute
Pfizer
Texas A&M University

Research output: Contribution to journal › Article › peer-review

10 Citations (Scopus)

Abstract

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 [IC₅₀] 3.6 μM) without cytotoxicity against eukaryotic cells (IC₅₀ 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.

Original language	English
Article number	e01205-17
Journal	Antimicrobial Agents and Chemotherapy
Volume	61
Issue number	9
Early online date	24 Aug 2017
DOIs	https://doi.org/10.1128/AAC.01205-17
Publication status	Published - 1 Sept 2017
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antimicrobial
Antitubercular
Drug resistance

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10.1128/AAC.01205-17Licence: CC BY

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title = "A novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro",

abstract = "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 [IC50] 3.6 μM) without cytotoxicity against eukaryotic cells (IC50 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.",

keywords = "Antimicrobial, Antitubercular, Drug resistance",

author = "Nipul Patel and Theresa O{\textquoteright}Malley and Zhang, \{Yong Kang\} and Yi Xia and Bjorn Sunde and Lindsay Flint and Aaron Korkegian and Ioerger, \{Thomas R.\} and Jim Sacchettini and Alley, \{M. R.K.\} and Tanya Parish",

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doi = "10.1128/AAC.01205-17",

language = "English",

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T1 - A novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro

AU - Patel, Nipul

AU - O’Malley, Theresa

AU - Zhang, Yong Kang

AU - Xia, Yi

AU - Sunde, Bjorn

AU - Flint, Lindsay

AU - Korkegian, Aaron

AU - Ioerger, Thomas R.

AU - Sacchettini, Jim

AU - Alley, M. R.K.

AU - Parish, Tanya

PY - 2017/9/1

Y1 - 2017/9/1

N2 - 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 [IC50] 3.6 μM) without cytotoxicity against eukaryotic cells (IC50 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.

AB - 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 [IC50] 3.6 μM) without cytotoxicity against eukaryotic cells (IC50 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.

KW - Antimicrobial

KW - Antitubercular

KW - Drug resistance

U2 - 10.1128/AAC.01205-17

DO - 10.1128/AAC.01205-17

M3 - Article

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AN - SCOPUS:85028341795

SN - 0066-4804

VL - 61

JO - Antimicrobial Agents and Chemotherapy

JF - Antimicrobial Agents and Chemotherapy

IS - 9

M1 - e01205-17

ER -

A novel 6-benzyl ether benzoxaborole is active against mycobacterium tuberculosis in vitro

Abstract

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Keywords

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