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Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
Wilson, Colin R; Gessner, Richard K; Moosa, Atica; Seldon, Ronnett; Warner, Digby F; Mizrahi, Valerie; Soares de Melo, Candice; Simelane, Sandile B; Nchinda, Aloysius; Abay, Efrem; Taylor, Dale; Njoroge, Mathew; Brunschwig, Christel; Lawrence, Nina; Boshoff, Helena I M; Barry, Clifton E; Sirgel, Frederick A; van Helden, Paul; Harris, C John; Gordon, Richard; Ghidelli-Disse, Sonja; Pflaumer, Hannah; Boesche, Markus; Drewes, Gerard; Sanz, Olalla; Santos, Gracia; Rebollo-Lopez, Maria José; Urones, Beatriz; Selenski, Carolyn; Lafuente-Monasterio, Maria Jose; Axtman, Matthew; Lelièvre, Joël; Ballell, Lluis; Mueller, Rudolf; Street, Leslie J; Ghorpade, Sandeep R; Chibale, Kelly.
Afiliação
  • Wilson CR; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Gessner RK; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Moosa A; SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.
  • Seldon R; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Warner DF; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
  • Mizrahi V; SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.
  • Soares de Melo C; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
  • Simelane SB; SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.
  • Nchinda A; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
  • Abay E; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Taylor D; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Njoroge M; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
  • Brunschwig C; Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
  • Lawrence N; Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
  • Boshoff HIM; Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
  • Barry CE; Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
  • Sirgel FA; Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
  • van Helden P; Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
  • Harris CJ; Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
  • Gordon R; DST/NRF Centre of Excellence for Biomedical TB Research, SA MRC Centre for TB Research, Division of Molecular Biology and Human Genetics, Faculty of Health Sciences, Stellenbosch University , 7505 Tygerberg, South Africa.
  • Ghidelli-Disse S; DST/NRF Centre of Excellence for Biomedical TB Research, SA MRC Centre for TB Research, Division of Molecular Biology and Human Genetics, Faculty of Health Sciences, Stellenbosch University , 7505 Tygerberg, South Africa.
  • Pflaumer H; CJH Consultants , Ford Cottage, South Weirs, Brockenhurst, Hampshire SO42 7UQ, U.K.
  • Boesche M; Strategic Health Innovation Partnerships (SHIP), South African Medical Research Council , Parow Valley, Cape Town, South Africa.
  • Drewes G; Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
  • Sanz O; Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
  • Santos G; Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
  • Rebollo-Lopez MJ; Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
  • Urones B; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Selenski C; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Lafuente-Monasterio MJ; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Axtman M; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Lelièvre J; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Ballell L; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Mueller R; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Street LJ; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Ghorpade SR; Diseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • Chibale K; Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
J Med Chem ; 60(24): 10118-10134, 2017 12 28.
Article em En | MEDLINE | ID: mdl-29148755
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Relação Estrutura-Atividade / Mycobacterium tuberculosis / Antituberculosos Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Relação Estrutura-Atividade / Mycobacterium tuberculosis / Antituberculosos Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2017 Tipo de documento: Article