ArticleJournal of medicinal chemistry2022
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.
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Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13citing papers in PubMed
–field-weighted citation impact
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Who cites it
13 citing papers in PubMed.
- Large-Scale Chemical-Genetic Interaction Profiling Identifies a Small-Molecule Inhibitor ofACS infectious diseases · 2026Article
- Integrating chemical, genetic, and feasibility assessments for anti-tubercular target validation.EMBO molecular medicine · 2026Review
- Article
- Discovery of 2,4,5-Substituted Benzoxazole Derivatives as Pks13 Inhibitors via the Scaffold Hopping Strategy.ACS infectious diseases · 2025Article
- The power of DNA-encoded chemical libraries in the battle against drug-resistant bacteria.RSC advances · 2025Review
- Identification of a Series Containing a Pentafluorophenyl Moiety That Targets Pks13 to Inhibit Growth ofACS infectious diseases · 2025Article
- Structure-based Virtual Screening and Hit Identification of Novel designed Quinazolin-4(3H)-one Derivatives as Antitubercular Agent against TargetsCurrent drug discovery technologies · 2025Article
- Inhibitors of the Thioesterase Activity ofACS infectious diseases · 2024Article
- Unlocking Opportunities forACS infectious diseases · 2024Review
- Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.Journal of medicinal chemistry · 2023Article
- Oxetanes in Drug Discovery Campaigns.Journal of medicinal chemistry · 2023Review
- In Silico Development of Novel Benzofuran-1,3,4-Oxadiazoles as Lead Inhibitors ofPharmaceuticals (Basel, Switzerland) · 2023Article
- An integrated computational approach towards novel drugs discovery against polyketide synthase 13 thioesterase domain of Mycobacterium tuberculosis.Scientific reports · 2023Article
Corrections and comments
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Authors and funding
40 authors.
Caroline WilsonDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Peter RayDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Fabio ZuccottoDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-3888-7423
Jorge HernandezDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Anup AggarwalDepartment of Biochemistry and Biophysics, Texas A&M University, College Station, Texas 77843, United States.
Claire MackenzieDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Nicola CaldwellDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Malcolm TaylorDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Margaret HuggettDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Michael MathiesonDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Dinakaran MurugesanDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Alasdair SmithDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Susan DavisDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Mattia CoccoDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Maloy K ParaiDepartment of Biochemistry and Biophysics, Texas A&M University, College Station, Texas 77843, United States.
Arjun AcharyaDepartment of Biochemistry and Biophysics, Texas A&M University, College Station, Texas 77843, United States.
Fabio TamakiDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Paul ScullionDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Ola EpemoluDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Jennifer RileyDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Laste StojanovskiDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
Eva Maria Lopez-RománGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Pedro Alfonso Torres-GómezGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Ana Maria ToledoGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Laura Guijarro-LopezGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Isabel CaminoGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Curtis A EngelhartDepartment of Microbiology and Immunology, Weill Cornell Medical College, New York, New York 10065, United States.
Dirk SchnappingerDepartment of Microbiology and Immunology, Weill Cornell Medical College, New York, New York 10065, United States.
Lisa M MassoudiMycobacteria Research Laboratories, Department of Microbiology, Immunology, and Pathology, Colorado State University, 200 W. Lake Street, Fort Collins, Colorado 80523-1682, United States.
Anne LenaertsMycobacteria Research Laboratories, Department of Microbiology, Immunology, and Pathology, Colorado State University, 200 W. Lake Street, Fort Collins, Colorado 80523-1682, United States.
Gregory T RobertsonMycobacteria Research Laboratories, Department of Microbiology, Immunology, and Pathology, Colorado State University, 200 W. Lake Street, Fort Collins, Colorado 80523-1682, United States.
Chris WalpoleStructural Genomics Consortium, Research Institute of the McGill University Health Centre, 1001 Boulevard Décarie, Site Glen Block E, ES1.1614, Montréal, Québec H4A 3J1, Canada.
David MatthewsStructural Genomics Consortium, Research Institute of the McGill University Health Centre, 1001 Boulevard Décarie, Site Glen Block E, ES1.1614, Montréal, Québec H4A 3J1, Canada.
David FloydStructural Genomics Consortium, Research Institute of the McGill University Health Centre, 1001 Boulevard Décarie, Site Glen Block E, ES1.1614, Montréal, Québec H4A 3J1, Canada.
James C SacchettiniDepartment of Biochemistry and Biophysics, Texas A&M University, College Station, Texas 77843, United States.ORCID 0000-0001-5767-2367
Kevin D ReadDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-8536-0130
Lourdes EncinasGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Robert H BatesGlobal Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.ORCID 0000-0003-1926-8114
Simon R GreenDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0001-5054-4792
Paul G WyattDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-0397-245X
Funding
Vulnerabilities in Mycobacterial Cell-Wall BiogenesisP01AI095208 · NIAID · UNIVERSITY OF CALIFORNIA-IRVINE · PI SACCHETTINI, JAMES C · 2012 to 2022
$19.8MNIAID NIH HHS P01 AI095208Wellcome Trust
Abstract
With increasing drug resistance in tuberculosis (TB) patient populations, there is an urgent need for new drugs. Ideally, new agents should work through novel targets so that they are unencumbered by preexisting clinical resistance to current treatments. Benzofuran
Indexed as
Antitubercular AgentsBacterial ProteinsBenzofuransCardiotoxicityDrug DiscoveryERG1 Potassium ChannelHeartHumansMicrobial Sensitivity TestsModels, MolecularMycobacterium tuberculosisPalmitoyl-CoA HydrolasePiperidinesPolyketide SynthasesStructure-Activity RelationshipAntitubercular AgentsBacterial ProteinsBenzofuransERG1 Potassium ChannelPalmitoyl-CoA HydrolasePiperidinespolyketide synthase Pks13, Mycobacterium tuberculosisPolyketide SynthasesTAM16 compound
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Registered trials
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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.