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2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

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Enzymes
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Tuberculosis drug discovery in the post‐post‐genomic era
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Towards a new combination therapy for tuberculosis with next generation benzothiazinones
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The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis
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Why are membrane targets discovered by phenotypic screens and genome sequencing in Mycobacterium tuberculosis?
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The BCG Moreau RD16 deletion inactivates a repressor reshaping transcription of an adjacent gene
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Quinoxaline chemistry. Part 13: 3-carboxy-2-benzylamino-substituted quinoxalines and N-[4-[(3-carboxyquinoxalin-2-yl) aminomethyl]benzoyl]-l-glutamates: synthesis and evaluation of in vitro anticancer activity
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The challenge of new drug discovery for tuberculosis
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Recombineering in Mycobacterium tuberculosis
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Drugs for bad bugs: confronting the challenges of antibacterial discovery
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Advances in the development of new tuberculosis drugs and treatment regimens
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The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis
inferredcites →https://doi.org/10.1073/pnas.1205735109openalex-snapshot
Structural basis of inhibition of Mycobacterium tuberculosis DprE1 by benzothiazinone inhibitors
inferredcites →https://doi.org/10.1073/pnas.1309171110openalex-snapshot
Identification of a small molecule with activity against drug-resistant and persistent tuberculosis
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Biosynthesis of D ‐arabinose in mycobacteria – a novel bacterial pathway with implications for antimycobacterial therapy
inferredcites →https://doi.org/10.1126/science.1171583openalex-snapshot
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis
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Dynamic Persistence of Antibiotic-Stressed Mycobacteria
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Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis
inferredcites →https://doi.org/10.1128/aac.00821-10openalex-snapshot
Simple Model for Testing Drugs against Nonreplicating Mycobacterium tuberculosis
inferredcites →https://doi.org/10.1128/aac.01125-12openalex-snapshot
Streptomycin-Starved Mycobacterium tuberculosis 18b, a Drug Discovery Tool for Latent Tuberculosis
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Resazurin Microtiter Assay Plate: Simple and Inexpensive Method for Detection of Drug Resistance in Mycobacterium tuberculosis
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Decaprenylphosphoryl Arabinofuranose, the Donor of the d -Arabinofuranosyl Residues of Mycobacterial Arabinan, Is Formed via a Two-Step Epimerization of Decaprenylphosphoryl Ribose
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125 years after Robert Koch's discovery of the tubercle bacillus: the new XDR-TB threat. Is “science” enough to tackle the epidemic?
inferredcites →https://doi.org/10.1371/journal.pone.0065080openalex-snapshot
Mycobacterium tuberculosis Rv3406 Is a Type II Alkyl Sulfatase Capable of Sulfate Scavenging
inferredcites →https://doi.org/10.1371/journal.ppat.1000645openalex-snapshot
High Content Screening Identifies Decaprenyl-Phosphoribose 2′ Epimerase as a Target for Intracellular Antimycobacterial Inhibitors
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DprE1 - from the Discovery to the Promising Tuberculosis Drug Target
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Tuberculosis Drugs: New Candidates and How to Find More
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Resistance in tuberculosis: what do we know and where can we go?
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Enzymes: a practical introduction to structure, mechanism, and data analysis

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

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Novel insight into the reaction of nitro, nitroso and hydroxylamino benzothiazinones and of benzoxacinones with Mycobacterium tuberculosis DprE1
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3D-QSAR and ADMET studies of morpholino-pyrimidine inhibitors of DprE1 from Mycobacterium tuberculosis
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In silico guided design of non-covalent inhibitors of DprE1: synthesis and biological evaluation
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Targeting drug-resistant Mycobacterium tuberculosis : an integrated computational approach to identify DprE2 inhibitors
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3,5-disubstituted pyridines with potent activity against drug-resistant Mycobacterium tuberculosis clinical isolates
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Molecular Mechanisms of MmpL3 Function and Inhibition
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Drug ReposER: a web server for predicting similar amino acid arrangements to known drug binding interfaces for potential drug repositioning
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Inhibiting Mycobacterium tuberculosis within and without
inferred← citeshttps://doi.org/10.1101/2021.12.04.471217openalex-snapshot
The veterinary anti-parasitic selamectin is a novel inhibitor of the mycobacterial DprE1 enzyme
inferred← citeshttps://doi.org/10.1126/scitranslmed.aal1803openalex-snapshot
Targeting protein biotinylation enhances tuberculosis chemotherapy
inferred← citeshttps://doi.org/10.1128/9781555819316.refsopenalex-snapshot
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Biochemical Characterization of Glutamate Racemase—A New Candidate Drug Target against Burkholderia cenocepacia Infections
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Gain of function in Mycobacterium bovis BCG Moreau due to loss of a transcriptional repressor
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An Overview of Recent Advances in Biological and Pharmaceutical Developments of Fluoro-containing Drugs
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Mycobacterial tuberculosis Enzyme Targets and their Inhibitors
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Mycobacterial Cell Wall: A Source of Successful Targets for Old and New Drugs
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Unveiling DprE1 as a Key Target in the Fight against Tuberculosis: Insights and Perspectives on Developing Novel Antimicrobial Agents
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The Veterinary Anti-Parasitic Selamectin Is a Novel Inhibitor of the Mycobacterium tuberculosis DprE1 Enzyme
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Design, Synthesis, Antimycobacterial Evaluation, and In Silico Studies of 3-(Phenylcarbamoyl)-pyrazine-2-carboxylic Acids
inferred← citeshttps://doi.org/10.3390/molecules23030524openalex-snapshot
Virtual Screening of Small Molecular Inhibitors against DprE1
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Quinoxaline Moiety: A Potential Scaffold against Mycobacterium tuberculosis
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Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV
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Synthesis, Activity, Toxicity, and In Silico Studies of New Antimycobacterial N-Alkyl Nitrobenzamides
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Deciphering antimycobacterial activity of cyclophostin/cyclipostins analogs and oxadiazolones derivatives, two new promising family compounds in the treatment of tuberculosis and mycobacterial-related diseases
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