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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.
Afiliación
  • Patel N; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • O'Malley T; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Zhang YK; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Xia Y; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Sunde B; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Flint L; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Korkegian A; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Ioerger TR; Texas A&M University, College Station, Texas, USA.
  • Sacchettini J; Texas A&M University, College Station, Texas, USA.
  • Alley MRK; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Parish T; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA tanya.parish@idri.org.
Antimicrob Agents Chemother ; 61(9)2017 09.
Article en En | MEDLINE | ID: mdl-28674058
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tuberculosis Pulmonar / Tuberculosis Resistente a Múltiples Medicamentos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: Antimicrob Agents Chemother Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tuberculosis Pulmonar / Tuberculosis Resistente a Múltiples Medicamentos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: Antimicrob Agents Chemother Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos