ArticlePloS one2014
Bactericidal activity of an imidazo[1, 2-a]pyridine using a mouse M. tuberculosis infection model.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 58 citations in OpenAlex.
- Exploration of imidazothiazole and imidazopyrimidine carboxamides for enhanced antitubercular activity.Bioorganic & medicinal chemistry letters · 2026Article
- Imidazo[1,2‑ACS omega · 2026Review
- Syntheses and studies of deuterated Imdiazo[1,2-a]pyridine-3-carboxamides with potent anti-tuberculosis activity and improved metabolic properties.Bioorganic chemistry · 2022Article
- Targeting the cytochrome bcMolecular diversity · 2022Review
- Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-RSC medicinal chemistry · 2022Article
- On drug discovery against infectious diseases and academic medicinal chemistry contributions.Beilstein journal of organic chemistry · 2022Article
- Design and Syntheses of New Antibiotics Inspired by Nature's Quest for Iron in an Oxidative Climate.Accounts of chemical research · 2021Review
- Design, synthesis, and biological evaluation of novel imidazo[1,2-a]pyridinecarboxamides as potent anti-tuberculosis agents.Chemical biology & drug design · 2020Article
- Host cytosolic RNA sensing pathway promotes T Lymphocyte-mediated mycobacterial killing in macrophages.PLoS pathogens · 2020Article
- Terminal Respiratory Oxidases: A Targetables Vulnerability of Mycobacterial Bioenergetics?Frontiers in cellular and infection microbiology · 2020Review
- Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds.PloS one · 2020Article
- Extracellular vesicles deliverEMBO reports · 2019Article
- Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.Journal of medicinal chemistry · 2018Article
- Imidazopyridine Compounds Inhibit Mycobacterial Growth by Depleting ATP Levels.Antimicrobial agents and chemotherapy · 2018Article
- Mycobacterial Membrane Proteins QcrB and AtpE: Roles in Energetics, Antibiotic Targets, and Associated Mechanisms of Resistance.The Journal of membrane biology · 2018Article
- Predictive Model for Site-Selective Aryl and Heteroaryl C-H Functionalization via Organic Photoredox Catalysis.Journal of the American Chemical Society · 2017Article
- Preparation and Evaluation of Potent Pentafluorosulfanyl-Substituted Anti-Tuberculosis Compounds.ChemMedChem · 2017Article
- Identification ofACS medicinal chemistry letters · 2016Article
- Ι₂-mediated amination/cyclization of ketones with 2-aminopyridines under high-speed ball milling: solvent- and metal-free synthesis of 2,3-substituted imidazo[1,2-a]pyridines and zolimidine.Molecular diversity · 2016Article
- Imidazo[1,2-a]Pyridine-3-Carboxamides Are Active Antimicrobial Agents against Mycobacterium avium Infection In Vivo.Antimicrobial agents and chemotherapy · 2016Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Tuberculosis remains a global threat due in part to the long treatment regimen and the increased prevalence of drug resistant M. tuberculosis strains. Therefore, new drug regimens are urgently required to combat this deadly disease. We previously synthesized and evaluated a series of new anti-tuberculosis compounds which belong to the family of imidazo[1,2-a]pyridines. This family of compounds showed low nM MIC (minimal inhibitory concentration) values against M. tuberculosis in vitro. In this study, a derivative of imidazo[1,2-a]pyridines, (N-(4-(4-chlorophenoxy)benzyl)-2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamide) (ND-09759), was selected as a promising lead compound to determine its protective efficacy using a mouse infection model. Pharmacokinetic analysis of ND-09759 determined that at a dosage of 30 mg/kg mouse body weight (PO) gave a maximum serum drug concentration (Cmax) of 2.9 µg/ml and a half-life of 20.1 h. M. tuberculosis burden in the lungs and spleens was significantly decreased in mice treated once daily 6 days per week for 4-weeks with ND-09759 compared to untreated mice and this antibiotic activity was equivalent to isoniazid (INH) and rifampicin (RMP), two first-line anti-TB drugs. We observed slightly higher efficacy when using a combination of ND-09759 with either INH or RMP. Finally, the histopathological analysis revealed that infected mice treated with ND-09759 had significantly reduced inflammation relative to untreated mice. In conclusion, our findings indicate ND-09759 might be a potent candidate for the treatment of active TB in combination with current standard anti-TB drugs.
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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.