ArticleChemMedChem2014
Biological evaluation of potent triclosan-derived inhibitors of the enoyl-acyl carrier protein reductase InhA in drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis.
Article in ChemMedChem, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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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
19 citing papers in PubMed, 34 citations in OpenAlex.
- Targeting InhA for Tuberculosis Therapy: A Review of Recent Advances in Enzyme Inhibition and Drug Development.Current drug targets · 2026Review
- Is Mycobacterial InhA a Suitable Target for Rational Drug Design?ChemMedChem · 2025Review
- Rational design and microwave-promoted synthesis of triclosan-based dimers: targeting InhA for anti-mycobacterial profiling.Royal Society open science · 2024Article
- Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme andMolecules (Basel, Switzerland) · 2024Article
- Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation withFuture medicinal chemistry · 2024Article
- Tailoring selective triclosan azo-adducts: Design, synthesis, and anti-mycobacterial evaluation.Heliyon · 2023Article
- Recent Discoveries of Nitrogen-Containing Heterocyclic Compounds as InhA Inhibitors againstInfectious disorders drug targets · 2022Article
- New InhA Inhibitors Based on Expanded Triclosan andPharmaceuticals (Basel, Switzerland) · 2021Article
- Exploring the chemical space of 1,2,3-triazolyl triclosan analogs for discovery of new antileishmanial chemotherapeutic agents.RSC medicinal chemistry · 2021Article
- Computational Approaches to Identify Molecules Binding toACS omega · 2020Article
- In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors.Molecules (Basel, Switzerland) · 2020Article
- Antitubercular Triazines: Optimization and Intrabacterial Metabolism.Cell chemical biology · 2020Article
- Intrabacterial Metabolism Obscures the Successful Prediction of an InhA Inhibitor ofACS infectious diseases · 2019Article
- Structure-Based Design and in Silico Screening of Virtual Combinatorial Library of Benzamides Inhibiting 2-trans Enoyl-Acyl Carrier Protein Reductase ofInternational journal of molecular sciences · 2019Article
- Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Evaluating the Contribution of Transition-State Destabilization to Changes in the Residence Time of Triazole-Based InhA Inhibitors.Journal of the American Chemical Society · 2017Article
- Triclosan-induced genes Rv1686c-Rv1687c and Rv3161c are not involved in triclosan resistance in Mycobacterium tuberculosis.Scientific reports · 2016Article
- A virtual screen discovers novel, fragment-sized inhibitors of Mycobacterium tuberculosis InhA.Journal of chemical information and modeling · 2015Article
- New therapeutic strategies forExpert review of anti-infective therapyReview
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 1 country.
Funding
Abstract
New triclosan (TRC) analogues were evaluated for their activity against the enoyl-acyl carrier protein reductase InhA in Mycobacterium tuberculosis (Mtb). TRC is a well-known inhibitor of InhA, and specific modifications to its positions 5 and 4' afforded 27 derivatives; of these compounds, seven derivatives showed improved potency over that of TRC. These analogues were active against both drug-susceptible and drug-resistant Mtb strains. The most active compound in this series, 4-(n-butyl)-1,2,3-triazolyl TRC derivative 3, had an MIC value of 0.6 μg mL(-1) (1.5 μM) against wild-type Mtb. At a concentration equal to its MIC, this compound inhibited purified InhA by 98 %, and showed an IC50 value of 90 nM. Compound 3 and the 5-methylisoxazole-modified TRC 14 were able to inhibit the biosynthesis of mycolic acids. Furthermore, mc(2) 4914, an Mtb strain overexpressing inhA, was found to be less susceptible to compounds 3 and 14, supporting the notion that InhA is the likely molecular target of the TRC derivatives presented herein.
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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.