ArticleJournal of medicinal chemistry2017
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
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Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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9citing papers in PubMed
1.9field-weighted citation impact, top 14% of its field
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Who cites it
9 citing papers in PubMed, 24 citations in OpenAlex.
- 1,3-Diarylpyrazolyl-acylsulfonamides Target HadAB/BC Complex inACS infectious diseases · 2022Article
- The multi-target aspect of an MmpL3 inhibitor: The BM212 series of compounds bind EthR2, a transcriptional regulator of ethionamide activation.Cell surface (Amsterdam, Netherlands) · 2021Article
- Strategies to Combat Multi-Drug Resistance in Tuberculosis.Accounts of chemical research · 2021Review
- Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.Journal of medicinal chemistry · 2021Article
- Molecule Property Analyses of Active Compounds forJournal of medicinal chemistry · 2020Review
- Solvent-Free Iron(III) Chloride-Catalyzed Direct Amidation of Esters.Molecules (Basel, Switzerland) · 2020Article
- Biological Profiling Enables Rapid Mechanistic Classification of Phenotypic Screening Hits and Identification of KatG Activation-Dependent Pyridine Carboxamide Prodrugs With Activity AgainstFrontiers in cellular and infection microbiology · 2020Article
- ADME prediction with KNIME:ADMET & DMPK · 2020Article
- Improved Prediction of Aqueous Solubility of Novel Compounds by Going Deeper With Deep Learning.Frontiers in oncology · 2020Article
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Authors and funding
37 authors at 6 institutions in 5 countries.
Colin R WilsonDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Richard K GessnerDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Atica MoosaSAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.
Ronnett SeldonDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Digby F WarnerSAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.
Valerie MizrahiSAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town , Rondebosch 7701, South Africa.ORCID 0000-0003-4824-9115
Candice Soares de MeloDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Sandile B SimelaneDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Aloysius NchindaDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Efrem AbayDepartment of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
Dale TaylorDepartment of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
Mathew NjorogeDepartment of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
Christel BrunschwigDepartment of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
Nina LawrenceDepartment of Medicine, Division of Clinical Pharmacology, Drug Discovery and Development Centre (H3D), University of Cape Town , Observatory, 7925, South Africa.
Helena I M BoshoffTuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
Clifton E BarryTuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
Frederick A SirgelDST/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.
Paul van HeldenDST/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.
C John HarrisCJH Consultants , Ford Cottage, South Weirs, Brockenhurst, Hampshire SO42 7UQ, U.K.
Richard GordonStrategic Health Innovation Partnerships (SHIP), South African Medical Research Council , Parow Valley, Cape Town, South Africa.
Sonja Ghidelli-DisseCellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
Hannah PflaumerCellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
Markus BoescheCellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
Gerard DrewesCellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, Heidelberg 69117, Germany.
Olalla SanzDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Gracia SantosDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Maria José Rebollo-LopezDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Beatriz UronesDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Carolyn SelenskiDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Maria Jose Lafuente-MonasterioDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Matthew AxtmanDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Joël LelièvreDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Lluis BallellDiseases of the Developing World, GlaxoSmithKline , Calle Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Rudolf MuellerDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Leslie J StreetDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.
Sandeep R GhorpadeDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.ORCID 0000-0002-9311-1572
Kelly ChibaleDepartment of Chemistry, Drug Discovery and Development Centre (H3D), University of Cape Town , Rondebosch 7701, South Africa.ORCID 0000-0002-1327-4727
University of Cape Town · ZAGlaxoSmithKline (Spain) · ESSouth African Medical Research Council · ZAGlaxoSmithKline (Germany) · DENational Institutes of Health · USBrockenhurst College · GB
Funding
Development Of New Chemotherapeutics For TuberculosisZIAAI000693 · NIAID · NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES · PI BARRY, CLIFTON · 2009 to 2025
$20.1MAbstract
A BioFocus DPI SoftFocus library of ∼35 000 compounds was screened against Mycobacterium tuberculosis (Mtb) in order to identify novel hits with antitubercular activity. The hits were evaluated in biology triage assays to exclude compounds suggested to function via frequently encountered promiscuous mechanisms of action including inhibition of the QcrB subunit of the cytochrome bc
Indexed as
Structure-Activity RelationshipAdministration, OralAnimalsAntitubercular AgentsBlood ProteinsDrug StabilityHigh-Throughput Screening AssaysHumansMaleMice, Inbred C57BLMicrosomes, LiverMycobacterium tuberculosisProteomicsPyrimidinesSmall Molecule Libraries2-aminopyrimidineAntitubercular AgentsBlood ProteinsPyrimidinesSmall Molecule Libraries
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.