ArticleThe Journal of antimicrobial chemotherapy2017
Evaluation of minor groove binders (MGBs) as novel anti-mycobacterial agents and the effect of using non-ionic surfactant vesicles as a delivery system to improve their efficacy.
Article in The Journal of antimicrobial chemotherapy, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 23 citations in OpenAlex.
- Meta-Analysis of Drug Delivery Approaches for Treating Intracellular Infections.Pharmaceutical research · 2022Pooled it
- Strathclyde Minor Groove Binders Bearing Amidine Tail Groups are Effective against Gram-Positive Bacterial Pathogens.ACS infectious diseases · 2026Article
- Strathclyde minor groove binders (S-MGBs) with activity against Acanthamoeba castellanii.The Journal of antimicrobial chemotherapy · 2024Article
- The allure of targets for novel drugs.RSC medicinal chemistry · 2024Review
- MptpB Inhibitor Improves the Action of Antibiotics againstACS infectious diseases · 2024Article
- Dissociation kinetics of small-molecule inhibitors in Escherichia coli is coupled to physiological state of cells.Communications biology · 2023Article
- Insights into the Spectrum of Activity and Mechanism of Action of MGB-BP-3.ACS infectious diseases · 2022Article
- Selective Anti-Leishmanial Strathclyde Minor Groove Binders Using an N-Oxide Tail-Group Modification.International journal of molecular sciences · 2022Article
- Multitargeted anti-infective drugs: resilience to resistance in the antimicrobial resistance era.Future drug discovery · 2022Review
- Intranasally administered S-MGB-364 displays antitubercular activity and modulates the host immune response to Mycobacterium tuberculosis infection.The Journal of antimicrobial chemotherapy · 2022Article
- Evaluation of Berberine as an Adjunct to TB Treatment.Frontiers in immunology · 2021Article
- SelectiveMedChemComm · 2019Article
- Recent developments in compounds acting in the DNA minor groove.MedChemComm · 2019Review
- Activity of DNA-targeted C8-linked pyrrolobenzodiazepine-heterocyclic polyamide conjugates against aerobically and hypoxically grown Mycobacterium tuberculosis under acidic and neutral conditions.The Journal of antibiotics · 2018Article
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 2 countries.
Funding
Abstract
objectivesThe slow development of major advances in drug discovery for the treatment of Mycobacterium tuberculosis (Mtb) infection suggests a compelling need for evaluation of more effective drug therapies against TB. New classes of drugs are constantly being evaluated for anti-mycobacterial activity with currently a very limited number of new drugs approved for TB treatment. Minor groove binders (MGBs) have previously revealed promising antimicrobial activity against various infectious agents; however, they have not yet been screened against Mtb.
methodsThe mycobactericidal activity of 96 MGB compounds against Mtb was determined using an H37Rv-GFP microplate assay. MGB hits were screened for their intracellular mycobactericidal efficacy against the clinical Beijing Mtb strain HN878 in bone-marrow-derived macrophages using standard cfu counting. Cell viability was assessed by CellTiter-Blue assays. Selected MGBs were encapsulated into non-ionic surfactant vesicles (NIVs) for drug delivery system evaluation.
resultsH37Rv-GFP screening yielded a hit-list of seven compounds at an MIC99 of between 0.39 and 1.56 μM. MGB-362 and MGB-364 displayed intracellular mycobactericidal activity against Mtb HN878 at an MIC50 of 4.09 and 4.19 μM, respectively, whilst being non-toxic. Subsequent encapsulation into NIVs demonstrated a 1.6- and 2.1-fold increased intracellular mycobacterial activity, similar to that of rifampicin when compared with MGB-alone formulation.
conclusionsMGB anti-mycobacterial activities together with non-toxic properties indicate that MGB compounds constitute an important new class of drug/chemical entity, which holds promise in future anti-TB therapy. Furthermore, the ability of NIVs to better deliver entrapped MGB compounds to an intracellular Mtb infection suggests further preclinical evaluation is warranted.
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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.