ArticlePloS one2013
A dual read-out assay to evaluate the potency of compounds active against Mycobacterium tuberculosis.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 99 papers.
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Who cites it
99 citing papers in PubMed.
- 4‑Aminoalkylquinolines as Potent Antitubercular Agents Targeting the Cytochrome bcACS medicinal chemistry letters · 2026Article
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- Scaffold Hopping Strategy toward New 4‑Aminoquinazolines Active Against Extracellular and Intracellular.ACS medicinal chemistry letters · 2025Article
- New Triazolopyrimidines with Improved Activity againstACS medicinal chemistry letters · 2025Article
- Deep learning-driven bacterial cytological profiling to determine antimicrobial mechanisms inProceedings of the National Academy of Sciences of the United States of America · 2025Article
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- 8-Hydroxyquinoline Series Exerts Bactericidal Activity againstACS infectious diseases · 2024Article
- Ethambutol and meropenem/clavulanate synergy promotes enhanced extracellular and intracellular killing ofAntimicrobial agents and chemotherapy · 2024Article
- Benzene Amide Ether Scaffold is Active against Non-replicating and IntracellularACS infectious diseases · 2023Article
- Inoculum-dependent bactericidal activity of aMicrobiology (Reading, England) · 2023Article
- Deletion of Rv2571c confers resistance to arylamide compounds inAntimicrobial agents and chemotherapy · 2023Article
- Inoculum-dependent bactericidal activity of abioRxiv : the preprint server for biology · 2023Article
- Identification of 2-Amino Benzothiazoles with Bactericidal Activity against Mycobacterium tuberculosis.Microbiology spectrum · 2023Article
- Article
- Characterizing in vivo loss of virulence of an HN878 Mycobacterium tuberculosis isolate from a genetic duplication event.Tuberculosis (Edinburgh, Scotland) · 2022Article
- Syntheses and studies of deuterated Imdiazo[1,2-a]pyridine-3-carboxamides with potent anti-tuberculosis activity and improved metabolic properties.Bioorganic chemistry · 2022Article
- Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening.Scientific reports · 2022Article
- Chemical Exploration of a Highly Selective Scaffold with Activity against IntracellularMicrobiology spectrum · 2022Article
- New Quinoline-Urea-Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Triazolopyrimidines Target Aerobic Respiration in Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 2022Article
39 more citing papers are in PubMed but not listed here.
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Authors and funding
8 authors.
Funding
Abstract
Tuberculosis is a serious global health problem caused by the bacterium Mycobacterium tuberculosis. There is an urgent need for discovery and development of new treatments, but this can only be accomplished through rapid and reproducible M. tuberculosis assays designed to identify potent inhibitors. We developed an automated 96-well assay utilizing a recombinant strain of M. tuberculosis expressing a far-red fluorescent reporter to determine the activity of novel compounds; this allowed us to measure growth by monitoring both optical density and fluorescence. We determined that optical density and fluorescence were correlated with cell number during logarithmic phase growth. Fluorescence was stably maintained without antibiotic selection over 5 days, during which time cells remained actively growing. We optimized parameters for the assay, with the final format being 5 days' growth in 96-well plates in the presence of 2% w/v DMSO. We confirmed reproducibility using rifampicin and other antibiotics. The dual detection method allows for a reproducible calculation of the minimum inhibitory concentration (MIC), at the same time detecting artefacts such as fluorescence quenching or compound precipitation. We used our assay to confirm anti-tubercular activity and establish the structure activity relationship (SAR) around the imidazo[1,2-a]pyridine-3-carboxamides, a promising series of M. tuberculosis inhibitors.
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Registered trials
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