ArticlePharmaceuticals (Basel, Switzerland)2021
New InhA Inhibitors Based on Expanded Triclosan and
Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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
9 citing papers in PubMed, 31 citations in OpenAlex.
- Progress of anti-tuberculosis drug targets and novel therapeutic strategies.Frontiers in microbiology · 2025Review
- Article
- Antibacterial Prodrugs to Overcome Bacterial Antimicrobial Resistance.Pharmaceuticals (Basel, Switzerland) · 2024Review
- 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
- Triclosan: A Small Molecule with Controversial Roles.Antibiotics (Basel, Switzerland) · 2022Review
- Structural homology between 11 beta-hydroxysteroid dehydrogenase andFrontiers in endocrinology · 2022Article
- HowFrontiers in cellular and infection microbiology · 2022Review
- Recent Discoveries of Nitrogen-Containing Heterocyclic Compounds as InhA Inhibitors againstInfectious disorders drug targets · 2022Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
The emergence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) has reinforced the need for the development of new anti-TB drugs. The first line drug isoniazid inhibits InhA. This is a prodrug requiring activation by the enzyme KatG. Mutations in KatG have largely contributed to clinical isoniazid resistance. We aimed to design new 'direct' InhA inhibitors that obviate the need for activation by KatG, circumventing pre-existing resistance. In silico molecular modelling was used as part of a rational structure-based drug-design approach involving inspection of protein crystal structures of InhA:inhibitor complexes, including the broad spectrum antibiotic triclosan (TCS). One crystal structure exhibited the unusual presence of two triclosan molecules within the
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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.