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Towards a new combination therapy for tuberculosis with next generation benzothiazinones
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What this work says
Outgoing claims: the papers this work cites, builds on, or argues with.
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The challenge of new drug discovery for tuberculosis
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The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis
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Delamanid for Multidrug-Resistant Pulmonary Tuberculosis
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Insights from the complete genome sequence of Mycobacterium marinum on the evolution of Mycobacterium tuberculosis
inferredcites →https://doi.org/10.1111/j.1365-2958.2010.07277.xopenalex-snapshot
Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance
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A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis
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Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis
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Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis
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Clinical Isolates of Mycobacterium tuberculosis in Four European Hospitals Are Uniformly Susceptible to Benzothiazinones
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SQ109 Targets MmpL3, a Membrane Transporter of Trehalose Monomycolate Involved in Mycolic Acid Donation to the Cell Wall Core of Mycobacterium tuberculosis
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Zebrafish embryo screen for mycobacterial genes involved in the initiation of granuloma formation reveals a newly identified ESX-1 component
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OPC-67683, a Nitro-Dihydro-Imidazooxazole Derivative with Promising Action against Tuberculosis In Vitro and In Mice
What points at this work
Incoming claims: where this work appears in other papers’ reference lists and arguments.
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Solubility-driven optimization of benzothiopyranone salts leading to a preclinical candidate with improved pharmacokinetic properties and activity against Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.115539openalex-snapshot
Quinolone analogues of benzothiazinone: Synthesis, antitubercular structure-activity relationship and ADME profiling
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.115611openalex-snapshot
2,6-Disubstituted 7-(naphthalen-2-ylmethyl)-7H-purines as a new class of potent antitubercular agents inhibiting DprE1
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.115702openalex-snapshot
Targeting polyketide synthase 13 for the treatment of tuberculosis
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.115976openalex-snapshot
Benzothiozinone derivatives with anti-tubercular Activity−Further side chain investigation
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116559openalex-snapshot
DprE1 and Ddn as promising therapeutic targets in the development of novel anti-tuberculosis nitroaromatic drugs
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116829openalex-snapshot
Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility
inferred← citeshttps://doi.org/10.1016/j.ejmech.2025.117951openalex-snapshot
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade
inferred← citeshttps://doi.org/10.1016/j.ejmech.2026.118622openalex-snapshot
New antitubercular pretomanid analogues as potent payloads in polymeric micelles: Leveraging zebrafish assays to accelerate lead optimisation
inferred← citeshttps://doi.org/10.1016/j.ejmech.2026.118718openalex-snapshot
PROTACs as novel therapeutics against Mycobacterium tuberculosis: Current progress and future directions
inferred← citeshttps://doi.org/10.1016/j.ejps.2017.03.028openalex-snapshot
Anti-tubercular drug discovery: in silico implications and challenges
inferred← citeshttps://doi.org/10.1016/j.ejps.2017.05.053openalex-snapshot
Biopharmaceutic parameters, pharmacokinetics, transport and CYP-mediated drug interactions of IIIM-017: A novel nitroimidazooxazole analogue with anti-tuberculosis activity
inferred← citeshttps://doi.org/10.1016/j.ijmyco.2015.02.002openalex-snapshot
Benzothiazinone-piperazine derivatives as efficient Mycobacterium tuberculosis DNA gyrase inhibitors
inferred← citeshttps://doi.org/10.1016/j.ijpharm.2021.121369openalex-snapshot
Development of potent nanosized isatin-isonicotinohydrazide hybrid for management of Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.ijtb.2020.07.017openalex-snapshot
A review of recent advances in anti-tubercular drug development
inferred← citeshttps://doi.org/10.1016/j.insi.2025.100087openalex-snapshot
Synthetic and In Silico strategies toward DprE1 inhibitors: Advancing antitubercular therapies
inferred← citeshttps://doi.org/10.1016/j.isci.2026.115641openalex-snapshot
Oral milk exosome-PLGA nanoparticles enhance anti-tuberculosis efficacy of PBTZ169 and bedaquiline
inferred← citeshttps://doi.org/10.1016/j.jchromb.2022.123555openalex-snapshot
Optimized LC-MS/MS quantification of tuberculosis drug candidate macozinone (PBTZ169), its dearomatized Meisenheimer Complex and other metabolites, in human plasma and urine
inferred← citeshttps://doi.org/10.1016/j.jconrel.2020.08.022openalex-snapshot
In vitro and in vivo antitubercular activity of benzothiazinone-loaded human serum albumin nanocarriers designed for inhalation
inferred← citeshttps://doi.org/10.1016/j.jddst.2022.103690openalex-snapshot
Recent developments, challenges and future prospects in advanced drug delivery systems in the management of tuberculosis
inferred← citeshttps://doi.org/10.1016/j.jfluchem.2019.02.009openalex-snapshot
SYNTHESIS AND ANTITUBERCULAR EVALUATION OF FLUORINATED 2-CYCLOALKYLIMINO SUBSTITUTED 1,3-BENZOTHIAZIN-4-ONES
inferred← citeshttps://doi.org/10.1016/j.jgar.2019.06.013openalex-snapshot
In vitro interaction profiles of the new antitubercular drugs bedaquiline and delamanid with moxifloxacin against clinical Mycobacterium tuberculosis isolates
inferred← citeshttps://doi.org/10.1016/j.jiph.2022.08.016openalex-snapshot
An insight into the discovery, clinical studies, compositions, and patents of macozinone: A drug targeting the DprE1 enzyme of Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.jmgm.2020.107770openalex-snapshot
Virtual screening and free energy estimation for identifying Mycobacterium tuberculosis flavoenzyme DprE1 inhibitors
inferred← citeshttps://doi.org/10.1016/j.lfs.2021.119301openalex-snapshot
Comprehensive review on mechanism of action, resistance and evolution of antimycobacterial drugs
inferred← citeshttps://doi.org/10.1016/j.mencom.2020.07.007openalex-snapshot
Synthesis of novel 8-nitro-substituted 1,3-benzothiazin-4-ones
inferred← citeshttps://doi.org/10.1016/j.meomic.2023.100022openalex-snapshot
Molecular diagnostics and potential therapeutic options for mycobacterium tuberculosis: Where we stand
inferred← citeshttps://doi.org/10.1016/j.mib.2017.11.017openalex-snapshot
Host–pathogen systems for early drug discovery against tuberculosis
inferred← citeshttps://doi.org/10.1016/j.mib.2018.02.006openalex-snapshot
Priming the tuberculosis drug pipeline: new antimycobacterial targets and agents
inferred← citeshttps://doi.org/10.1016/j.micinf.2024.105376openalex-snapshot
Efficacy of macozinone in mice with genetically diverse susceptibility to Mycobacterium tuberculosis infection
inferred← citeshttps://doi.org/10.1016/j.micpath.2024.107074openalex-snapshot
Advancements and challenges in tuberculosis drug discovery: A comprehensive overview
inferred← citeshttps://doi.org/10.1016/j.micres.2024.127675openalex-snapshot
Modulators targeting protein-protein interactions in Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.molstruc.2021.131419openalex-snapshot
Structural elucidation of the antitubercular benzothiazinone BTZ043: A combined X-ray, variable temperature NMR and DFT study
inferred← citeshttps://doi.org/10.1016/j.molstruc.2024.140072openalex-snapshot
Design, synthesis and molecular docking study of novel quinoline–triazole molecular hybrids as anticancer agents
inferred← citeshttps://doi.org/10.1016/j.molstruc.2025.141594openalex-snapshot
Quinazolinone-linked triazole conjugates: Synthesis, biological evaluation, and in silico studies
inferred← citeshttps://doi.org/10.1016/j.molstruc.2025.144674openalex-snapshot
Exploring quinazolinone linked 1,4-disustituted mono- and bis-1,2,3-triazole derivatives: A combined synthetic, anticancer, and molecular docking study
inferred← citeshttps://doi.org/10.1016/j.molstruc.2026.147551openalex-snapshot
Synthesis, Characterization, In Silico Studies, and Biological Evaluation of Pyrazine-2-carbohydrazide-Derived Azetidinone Hybrids as Potential Antitubercular Agents
inferred← citeshttps://doi.org/10.1016/j.pharep.2017.09.001openalex-snapshot
Novel compounds targeting InhA for TB therapy
inferred← citeshttps://doi.org/10.1016/j.trsl.2020.03.007openalex-snapshot
New tuberculosis drug targets, their inhibitors, and potential therapeutic impact
inferred← citeshttps://doi.org/10.1016/j.tube.2016.08.002openalex-snapshot
Recent developments in genomics, bioinformatics and drug discovery to combat emerging drug-resistant tuberculosis
inferred← citeshttps://doi.org/10.1016/j.tube.2023.102350openalex-snapshot
Discovery and biological evaluation of an adamantyl-amide derivative with likely MmpL3 inhibitory activity
inferred← citeshttps://doi.org/10.1016/j.tube.2025.102654openalex-snapshot
In vitro and in vivo activities of a novel benzothiopyranone candidate NTB-3119M against Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1016/j.xcrp.2023.101520openalex-snapshot
Integrating multi-modal deep learning on knowledge graph for the discovery of synergistic drug combinations against infectious diseases
inferred← citeshttps://doi.org/10.1017/s0031182016002377openalex-snapshot
Mycobacterial cell wall biosynthesis: a multifaceted antibiotic target
inferred← citeshttps://doi.org/10.1021/acs.chemrev.7b00602openalex-snapshot
Hit Generation in TB Drug Discovery: From Genome to Granuloma
inferred← citeshttps://doi.org/10.1021/acs.jafc.2c07312openalex-snapshot
Comparative Physicochemical and Biochemical Characterization of Small-Molecule Glucosides
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.1c00263openalex-snapshot
Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.1c01049openalex-snapshot
Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.2c00098openalex-snapshot
Development of Predictive Classification Models for Whole Cell Antimycobacterial Activity of Benzothiazinones
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.2c00227openalex-snapshot
Tuberculosis Drug Discovery: Challenges and New Horizons
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.3c01703openalex-snapshot
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5b00608openalex-snapshot
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5b01699openalex-snapshot
Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure–Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c01100openalex-snapshot
Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c02429openalex-snapshot
Discovery, Design, and Synthesis of Novel 2-Benzyl-2,7-diazaspiro[3.5]nonane Benzothiazinones with Broad-Spectrum Antimycobacterial Activity
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c03770openalex-snapshot
Discovery of Potent Benzoselenazinone-Based DprE1 Inhibitors: A Novel Selenium-Containing Scaffold with Superior Anti-TB Activity and Pharmacokinetic Properties
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.7b00793openalex-snapshot
Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.7b01347openalex-snapshot
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b00281openalex-snapshot
Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b00777openalex-snapshot
Indolyl Azaspiroketal Mannich Bases Are Potent Antimycobacterial Agents with Selective Membrane Permeabilizing Effects and in Vivo Activity
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.9b00912openalex-snapshot
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β- d -ribofuranose 2′-Oxidase
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.9b01561openalex-snapshot
Mycobacterium tuberculosis Decaprenylphosphoryl-β- d -ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.9b02075openalex-snapshot
Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis
inferred← citeshttps://doi.org/10.1021/acs.molpharmaceut.1c00791openalex-snapshot
Machine Learning Models for Mycobacterium tuberculosis In Vitro Activity: Prediction and Target Visualization
inferred← citeshttps://doi.org/10.1021/acs.orglett.6c00343openalex-snapshot
Access to Se/S-Containing Heterocycles via Hexafluoroisopropanol-Mediated Tandem Wolff Rearrangement/Cyclization
inferred← citeshttps://doi.org/10.1021/acschembio.5b00237openalex-snapshot
DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization
inferred← citeshttps://doi.org/10.1021/acschembio.8b00790openalex-snapshot
Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria
inferred← citeshttps://doi.org/10.1021/acsinfecdis.0c00622openalex-snapshot
Design and Synthesis of Pyrano[3,2- b ]indolones Showing Antimycobacterial Activity
inferred← citeshttps://doi.org/10.1021/acsinfecdis.6b00102openalex-snapshot
The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis
inferred← citeshttps://doi.org/10.1021/acsinfecdis.9b00388openalex-snapshot
New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.1c00652openalex-snapshot
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.5b00424openalex-snapshot
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.7b00106openalex-snapshot
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.8b00634openalex-snapshot
Spirocyclic and Bicyclic 8-Nitrobenzothiazinones for Tuberculosis with Improved Physicochemical and Pharmacokinetic Properties
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.9b00308openalex-snapshot
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State
inferred← citeshttps://doi.org/10.1021/acsmedchemlett.9b00343openalex-snapshot
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity
inferred← citeshttps://doi.org/10.1021/acsomega.2c05307openalex-snapshot
Recent Advances of DprE1 Inhibitors against Mycobacterium tuberculosis : Computational Analysis of Physicochemical and ADMET Properties
inferred← citeshttps://doi.org/10.1021/acsomega.5c00871openalex-snapshot
Synthesis, Characterization, and Anti- TB Application of Redox-Active Ethyl Carbazate-Derivatized Phenanthroline and Its Silver Complexes
inferred← citeshttps://doi.org/10.1021/acsptsci.4c00558openalex-snapshot
A Comparative Pharmacokinetics Study of Orally and Intranasally Administered 8-Nitro-1,3-benzothiazin-4-one (BTZ043) Amorphous Drug Nanoparticles
inferred← citeshttps://doi.org/10.1021/cb5007163openalex-snapshot
2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1
inferred← citeshttps://doi.org/10.1021/jm5002937openalex-snapshot
Discovery of Pyrazolopyridones as a Novel Class of Noncovalent DprE1 Inhibitor with Potent Anti-Mycobacterial Activity
inferred← citeshttps://doi.org/10.1021/jm500571fopenalex-snapshot
Lead Optimization of 1,4-Azaindoles as Antimycobacterial Agents
inferred← citeshttps://doi.org/10.1021/jm5005978openalex-snapshot
4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity
inferred← citeshttps://doi.org/10.1021/mc-2022-vol57.ch14openalex-snapshot
MEDICINAL CHEMISTRY ENDEAVORS FOR THE DISCOVERY OF NOVEL TUBERCULOSIS DRUGS
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