ArticleEBioMedicine2016
Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor.
Article in EBioMedicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 81 citations in OpenAlex.
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- Optimizing the Antibiotic Potency and Metabolic Stability of Pyridomycin Using a Semisynthetic Approach.Journal of medicinal chemistry · 2026Article
- Natural Products with Potent Antimycobacterial Activity (2000-2024): A Review.Molecules (Basel, Switzerland) · 2025Review
- Isoniazid-rhodanine molecular hybrids: design, synthesis, antimycobacterial activity and computational validation.RSC advances · 2025Article
- Is Mycobacterial InhA a Suitable Target for Rational Drug Design?ChemMedChem · 2025Review
- Synthesis of Novel Thiazole/Thiadiazole Conjugates of Fluoroquinolones as Potent Antibacterial and Antimycobacterial Agents.Chemical biology & drug design · 2025Article
- Experimental and theoretical studies on antituberculosis activity of different benzimidazole derivatives.Heliyon · 2025Article
- Development ofMini reviews in medicinal chemistry · 2025Review
- Contribution of direct InhA inhibitors to novel drug regimens in a mouse model of tuberculosis.Antimicrobial agents and chemotherapy · 2024Article
- Discovery of novel and potent InhA direct inhibitors by ensemble docking-based virtual screening and biological assays.Journal of computer-aided molecular design · 2023Article
- Evaluating the Impact of the Tyr158 pBiochemistry · 2023Article
- Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs.Nature communications · 2022Article
- Binding Thermodynamics and Dissociation Kinetics Analysis Uncover the Key Structural Motifs of Phenoxyphenol Derivatives as the Direct InhA Inhibitors and the Hotspot Residues of InhA.International journal of molecular sciences · 2022Article
- Development of New Antimycobacterial Sulfonyl Hydrazones and 4-Methyl-1,2,3-thiadiazole-Based Hydrazone Derivatives.Antibiotics (Basel, Switzerland) · 2022Article
- Recent Discoveries of Nitrogen-Containing Heterocyclic Compounds as InhA Inhibitors againstInfectious disorders drug targets · 2022Article
- HowFrontiers in cellular and infection microbiology · 2022Review
- Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010-2020 Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Single-Cell Analysis of Mycobacteria Using Microfluidics and Time-Lapse Microscopy.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Antibiotics and resistance: the two-sided coin of the mycobacterial cell wall.Cell surface (Amsterdam, Netherlands) · 2020Review
Corrections and comments
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Authors and funding
30 authors at 7 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite being one of the first antitubercular agents identified, isoniazid (INH) is still the most prescribed drug for prophylaxis and tuberculosis (TB) treatment and, together with rifampicin, the pillars of current chemotherapy. A high percentage of isoniazid resistance is linked to mutations in the pro-drug activating enzyme KatG, so the discovery of direct inhibitors (DI) of the enoyl-ACP reductase (InhA) has been pursued by many groups leading to the identification of different enzyme inhibitors, active against Mycobacterium tuberculosis (Mtb), but with poor physicochemical properties to be considered as preclinical candidates. Here, we present a series of InhA DI active against multidrug (MDR) and extensively (XDR) drug-resistant clinical isolates as well as in TB murine models when orally dosed that can be a promising foundation for a future treatment.
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Registered trials
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.