ArticleChemMedChem2011
Pyrido[1,2-a]benzimidazole-based agents active against tuberculosis (TB), multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB.
Article in ChemMedChem, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed.
- BZD9L1 benzimidazole analogue hampers colorectal tumor progression by impeding angiogenesis.World journal of gastrointestinal oncology · 2023Article
- Facile synthesis and antimycobacterial activity of isoniazid, pyrazinamide and ciprofloxacin derivatives.Chemical biology & drug design · 2021Article
- Design, synthesis and evaluation of novel indole-2-carboxamides for growth inhibition ofRSC advances · 2021Article
- Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.European journal of medicinal chemistry · 2021Article
- Design, synthesis and antimycobacterial evaluation of novel adamantane and adamantanol analogues effective against drug-resistant tuberculosis.Bioorganic chemistry · 2021Article
- Pyrimido[1,2-Chemistry of heterocyclic compounds · 2021Article
- Design, synthesis, and biological evaluation of novel imidazo[1,2-a]pyridinecarboxamides as potent anti-tuberculosis agents.Chemical biology & drug design · 2020Article
- Design, synthesis, and biological evaluation of novel arylcarboxamide derivatives as anti-tubercular agents.RSC advances · 2020Article
- Challenging the Drug-Likeness Dogma for New Drug Discovery in Tuberculosis.Frontiers in microbiology · 2018Review
- Novel drug targets for Mycobacterium tuberculosis: 2-heterostyrylbenzimidazoles as inhibitors of cell wall protein synthesis.Chemistry Central journal · 2017Article
- Mutation of Rv2887, a marR-like gene, confers Mycobacterium tuberculosis resistance to an imidazopyridine-based agent.Antimicrobial agents and chemotherapy · 2015Article
- Metal-free arylation of ethyl acetoacetate with hypervalent diaryliodonium salts: an immediate access to diverse 3-aryl-4(1H)-quinolones.The Journal of organic chemistry · 2015Article
- Article
- Pyrosequencing for rapid detection of tuberculosis resistance in clinical isolates and sputum samples from re-treatment pulmonary tuberculosis patients.BMC infectious diseases · 2014Article
- Indoleamides are active against drug-resistant Mycobacterium tuberculosis.Nature communications · 2013Article
- Antituberculosis: synthesis and antimycobacterial activity of novel benzimidazole derivatives.BioMed research international · 2013Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The struggle against tuberculosis (TB) is still far from over. TB, caused by Mycobacterium tuberculosis, is one of the deadliest infections worldwide. Co-infection with human immunodeficiency virus (HIV) and the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) strains have further increased the burden for this disease. Herein, we report the discovery of 2-(4-chlorobenzyl)-3-methyl-1-oxo-1H,5H-pyrido[1,2-a]benzimidazole-4-carbonitrile as an effective antitubercular agent and the structural modifications of this molecule that have led to analogues with improved potency and lower toxicity. A number of these derivatives were also active at sub-micromolar concentrations against resistant TB strains and devoid of apparent toxicity to Vero cells, thereby underscoring their value as novel scaffolds for the development of new 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.