Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.

Sutherland, Hamish S; Tong, Amy S T; Choi, Peter J; Blaser, Adrian; Franzblau, Scott G; Cooper, Christopher B; Upton, Anna M; Lotlikar, Manisha; Denny, William A; Palmer, Brian D

Sutherland, Hamish S; Tong, Amy S T; Choi, Peter J; Blaser, Adrian; Franzblau, Scott G; Cooper, Christopher B; Upton, Anna M; Lotlikar, Manisha; Denny, William A; Palmer, Brian D.

Afiliação

Sutherland HS; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Tong AST; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Choi PJ; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Blaser A; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Franzblau SG; Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.
Cooper CB; Global Alliance for TB Drug Development, 40 Wall St, New York, NY 10005, USA.
Upton AM; Global Alliance for TB Drug Development, 40 Wall St, New York, NY 10005, USA.
Lotlikar M; Global Alliance for TB Drug Development, 40 Wall St, New York, NY 10005, USA.
Denny WA; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand. Electronic address: b.denny@auckland.
Palmer BD; Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.

Bioorg Med Chem ; 28(1): 115213, 2020 01 01.

Article em En | MEDLINE | ID: mdl-31810890

Assuntos

Antituberculosos/farmacologia; Diarilquinolinas/farmacologia; Mycobacterium tuberculosis/efeitos dos fármacos; Animais; Antituberculosos/síntese química; Antituberculosos/química; Diarilquinolinas/síntese química; Diarilquinolinas/química; Relação Dose-Resposta a Droga; Humanos; Testes de Sensibilidade Microbiana; Estrutura Molecular; Mycobacterium tuberculosis/crescimento & desenvolvimento; Relação Estrutura-Atividade

Palavras-chave

CFU, colony-forming units; HPLC, high-peformance liquid chromatography; LDA, lithium diisopropylamide; LORA, low oxygen recovery assay; LiTMP, lithium tetramethylpiperidide; M.tb, Mycobacterium tuberculosis; MABA, microplate alamar blue assay; MIC(90), minimum concentration for 90% inhibition; TB, tuberculosis; hERG, the alpha subunit of a K+ channel that contributes to the electrical activity of the heart

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Diarilquinolinas / Mycobacterium tuberculosis / Antituberculosos Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Nova Zelândia

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