ArticleJournal of enzyme inhibition and medicinal chemistry2017
Antimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VII
Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Structure-Activity Relationships of Hemocompatible Cationic 6-Azaindole Pyridinium Salts: Antimicrobial and Anticancer Activity.Molecules (Basel, Switzerland) · 2026Article
- HybridPharmaceuticals (Basel, Switzerland) · 2025Article
- Transforming Alzheimer's Treatment: Unveiling New Potential with Drug Repurposing Strategies.Current medicinal chemistry · 2025Review
- New insides into chimeric and hybrid azines derivatives with antifungal activity.Future medicinal chemistry · 2024Review
- Hybrid Azine Derivatives: A Useful Approach for Antimicrobial Therapy.Pharmaceutics · 2022Review
- Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Cyclodextrin Encapsulated pH Sensitive Dyes as Fluorescent Cellular Probes: Self-Aggregation and In Vitro Assessments.Molecules (Basel, Switzerland) · 2020Article
- Hybrid Quinoline-Sulfonamide Complexes (MMolecules (Basel, Switzerland) · 2020Article
- Microwave Assisted Reactions of Azaheterocycles Formedicinal Chemistry Applications.Molecules (Basel, Switzerland) · 2020Review
- Article
- Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification.Antibiotics (Basel, Switzerland) · 2019Article
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Authors and funding
4 authors.
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Abstract
A series of 13 compounds having a monoindolizine mono-salt skeleton was designed and synthesised in order to evaluate their antimycobacterial activity. The synthesis is efficient, involving only three steps: two alkylations and one 3 + 2 dipolar cycloaddition. The antimicrobial activity against Mycobacterium tuberculosis H37Rv grown under aerobic conditions was evaluated, eight compounds showing a very good antimycobacterial activity. SAR correlation reveals a certain influence of the R substituent from the para position of benzoyl moiety at position 3 of indolizine. The most active five compounds passed the second stage of anti-TB testing, the assay demonstrating that they are potent against both replicating and non-replicating Mtb, have a bactericidal mechanism of action, are active against drug-resistant Mtb strains, present a moderate to good activity against nontuberculous mycobacteria, a good intracellular activity, and a moderate to high cytotoxicity. For one compound showing a promising anti-TB profile, a complete ADMET study has been performed.
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