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Efficacy and Improved Resistance Potential of a Cofactor-Independent InhA Inhibitor of Mycobacterium tuberculosis in the C3HeB/FeJ Mouse Model.
Robertson, Gregory T; Ektnitphong, Victoria A; Scherman, Michael S; McNeil, Matthew B; Dennison, Devon; Korkegian, Aaron; Smith, Anthony J; Halladay, Jason; Carter, David S; Xia, Yi; Zhou, Yasheen; Choi, Wai; Berry, Pamela W; Mao, Weimin; Hernandez, Vincent; Alley, M R K; Parish, Tanya; Lenaerts, Anne J.
Afiliação
  • Robertson GT; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA gregory.robertson@colostate.edu.
  • Ektnitphong VA; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.
  • Scherman MS; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.
  • McNeil MB; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Dennison D; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Korkegian A; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Smith AJ; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.
  • Halladay J; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Carter DS; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Xia Y; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Zhou Y; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Choi W; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Berry PW; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Mao W; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Hernandez V; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Alley MRK; Anacor Pharmaceuticals, Palo Alto, California, USA.
  • Parish T; TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
  • Lenaerts AJ; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.
Antimicrob Agents Chemother ; 63(4)2019 04.
Article em En | MEDLINE | ID: mdl-30745397
ABSTRACT
AN12855 is a direct, cofactor-independent inhibitor of InhA in Mycobacterium tuberculosis In the C3HeB/FeJ mouse model with caseous necrotic lung lesions, AN12855 proved efficacious with a significantly lower resistance frequency than isoniazid. AN12855 drug levels were better retained in necrotic lesions and caseum where the majority of hard to treat, extracellular bacilli reside. Owing to these combined attributes, AN12855 represents a promising alternative to the frontline antituberculosis agent isoniazid.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Tuberculose Pulmonar / Compostos de Boro / Hidrocarbonetos Fluorados / Inibinas / Mycobacterium tuberculosis / Antituberculosos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Antimicrob Agents Chemother Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Tuberculose Pulmonar / Compostos de Boro / Hidrocarbonetos Fluorados / Inibinas / Mycobacterium tuberculosis / Antituberculosos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Antimicrob Agents Chemother Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos