ArticleBioorganic & medicinal chemistry2017
Design, synthesis and evaluation of indole-2-carboxamides with pan anti-mycobacterial activity.
Article in Bioorganic & medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
What it found
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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
39 citing papers in PubMed, 67 citations in OpenAlex.
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- Pre-formulation development of highly potent nontuberculous mycobacterial agents.Results in chemistry · 2025Article
- Identification of novel inhibitors targeting Mycobacterium abscessus InhA through virtual screening, docking, and molecular dynamic simulations.Scientific reports · 2025Article
- Activity of combinations of bactericidal and bacteriostatic compounds inFrontiers in microbiology · 2025Review
- Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme andMolecules (Basel, Switzerland) · 2024Article
- Recent advances in mycobacterial membrane protein large 3 inhibitor drug design for mycobacterial infections.Expert opinion on drug discovery · 2023Review
- Structural Determinants of Indole-2-carboxamides: Identification of Lead Acetamides with Pan Antimycobacterial Activity.Journal of medicinal chemistry · 2023Article
- Microbiological profile, preclinical pharmacokinetics and efficacy of CRS0393, a novel antimycobacterial agent targeting MmpL3.Tuberculosis (Edinburgh, Scotland) · 2023Article
- Why Matter Matters: Fast-TrackingMolecules (Basel, Switzerland) · 2022Review
- Design, Synthesis, and Biological Evaluation of Pyrrole-2-carboxamide Derivatives as Mycobacterial Membrane Protein Large 3 Inhibitors for Treating Drug-Resistant Tuberculosis.Journal of medicinal chemistry · 2022Article
- Proton transfer activity of the reconstitutedProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Mycobacterium abscessus drug discovery using machine learning.Tuberculosis (Edinburgh, Scotland) · 2022Article
- Indole: A promising scaffold for the discovery and development of potential anti-tubercular agents.Current research in pharmacology and drug discovery · 2022Review
- Article
- The Antimalarial Mefloquine Shows Activity againstInternational journal of molecular sciences · 2021Article
- Pipeline of anti-Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities.Medicinal research reviews · 2021Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Current treatment regimens for non-tuberculous mycobacteria (NTM) and tuberculosis (TB) generally require long duration of therapy with multiple drugs, some of which are broad spectrum antibiotics. Despite some advances in antimicrobial compounds, there remains a need in therapy for antibiotics with specific mycobacterial targets. It has been shown that MmpL3 is an essential transporter required for the translocation of mycolic acids to the mycobacterial cell envelope. Here, we synthesized a series of indole-2-carboxamides that inhibit MmpL3 and have potent pan-activity against mycobacterial species. The compounds were tested against several fast and slow-growing Mycobacterium species, including M. abscessus, M. massiliense, M. bolletii, M. chelonae, M. tuberculosis, M. avium, M. xenopi and M. smegmatis. The target of these indole-based compounds makes them selective for mycobacteria, while showing no clinically relevant bactericidal activity against S. aureus or P. aeruginosa. These compounds were tested against THP-1, a human-cell line, and showed minimal in vitro cytotoxicity and good selectivity indices. The data shown and discussed suggest that lead indole-2-carboxamides are strong contenders for further preclinical testing as NTM therapeutics.
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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.