Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

Author:

Wilson Colin R.1,Gessner Richard K.1,Moosa Atica2,Seldon Ronnett13,Warner Digby F.23,Mizrahi Valerie23ORCID,Soares de Melo Candice1,Simelane Sandile B.1,Nchinda Aloysius1,Abay Efrem4,Taylor Dale4,Njoroge Mathew4,Brunschwig Christel4,Lawrence Nina4,Boshoff Helena I. M.5,Barry Clifton E.5,Sirgel Frederick A.6,van Helden Paul6,Harris C. John7,Gordon Richard8,Ghidelli-Disse Sonja9,Pflaumer Hannah9,Boesche Markus9,Drewes Gerard9,Sanz Olalla10,Santos Gracia10,Rebollo-Lopez Maria José10,Urones Beatriz10,Selenski Carolyn10,Lafuente-Monasterio Maria Jose10,Axtman Matthew10,Lelièvre Joël10,Ballell Lluis10,Mueller Rudolf1,Street Leslie J.1,Ghorpade Sandeep R.1ORCID,Chibale Kelly1311ORCID

Affiliation:

1. Department of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa

2. SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town, Rondebosch 7701, South Africa

3. Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa

4. Department of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town, Observatory, 7925, South Africa

5. Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892, United States

6. 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

7. CJH Consultants, Ford Cottage, South Weirs, Brockenhurst, Hampshire SO42 7UQ, U.K.

8. Strategic Health Innovation Partnerships (SHIP), South African Medical Research Council, Parow Valley, Cape Town, South Africa

9. Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline, Meyerhofstrasse 1, Heidelberg 69117, Germany

10. Diseases of the Developing World, GlaxoSmithKline, Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain

11. South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa

Funder

Division of Intramural Research, National Institute of Allergy and Infectious Diseases

Bill and Melinda Gates Foundation

University of Cape Town

National Research Foundation

South African Medical Research Council

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference37 articles.

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