ArticleNature communications2013
Indoleamides are active against drug-resistant Mycobacterium tuberculosis.
Article in Nature communications, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 85 papers.
What it found
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Who cites it
85 citing papers in PubMed.
- Gaining insights into MmpL3: combining structural and computational approaches to unlock transport and inhibitor-binding mechanisms.Acta crystallographica. Section D, Structural biology · 2026Article
- Exploration of imidazothiazole and imidazopyrimidine carboxamides for enhanced antitubercular activity.Bioorganic & medicinal chemistry letters · 2026Article
- ACA kills Mycobacterium tuberculosis and M. bovis by targeting cell wall core assembling protein CpsA.Communications biology · 2025Article
- A bioluminescence-based chemical screen identifies a bactericidal naphthalene scaffold targeting MmpL3 inbioRxiv : the preprint server for biology · 2025Article
- Loss of the ESX-5 secretion locus inProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Review
- Pre-formulation development of highly potent nontuberculous mycobacterial agents.Results in chemistry · 2025Article
- Developing novel indoles as antitubercular agents and simulated annealing-based analysis of their binding with MmpL3.Future medicinal chemistry · 2025Article
- CRISPR Interference-Mediated Silencing of theAntibiotics (Basel, Switzerland) · 2024Article
- An update on the secretory functions of brown, white, and beige adipose tissue: Towards therapeutic applications.Reviews in endocrine & metabolic disorders · 2024Review
- Identification and optimization of pyridine carboxamide-based scaffold as a drug lead forAntimicrobial agents and chemotherapy · 2024Article
- TheMicrobiology spectrum · 2024Article
- Glutamine metabolism inhibition has dual immunomodulatory and antibacterial activities against Mycobacterium tuberculosis.Nature communications · 2023Article
- Revolutionizing control strategies against Mycobacterium tuberculosis infection through selected targeting of lipid metabolism.Cellular and molecular life sciences : CMLS · 2023Review
- Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents.European journal of medicinal chemistry · 2023Article
- Recent advances in mycobacterial membrane protein large 3 inhibitor drug design for mycobacterial infections.Expert opinion on drug discovery · 2023Review
- Molecular Mechanisms of MmpL3 Function and Inhibition.Microbial drug resistance (Larchmont, N.Y.) · 2023Review
- Tuberculosis: Pathogenesis, Current Treatment Regimens and New Drug Targets.International journal of molecular sciences · 2023Review
- Structural Determinants of Indole-2-carboxamides: Identification of Lead Acetamides with Pan Antimycobacterial Activity.Journal of medicinal chemistry · 2023Article
- Expanding the knowledge around antitubercular 5-(2-aminothiazol-4-yl)isoxazole-3-carboxamides: Hit-to-lead optimization and release of a novel antitubercular chemotype via scaffold derivatization.European journal of medicinal chemistry · 2023Article
25 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Responsible for nearly two million deaths each year, the infectious disease tuberculosis remains a serious global health challenge. The emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis confounds control efforts, and new drugs with novel molecular targets are desperately needed. Here we describe lead compounds, the indoleamides, with potent activity against both drug-susceptible and drug-resistant strains of M. tuberculosis by targeting the mycolic acid transporter MmpL3. We identify a single mutation in mmpL3, which confers high resistance to the indoleamide class while remaining susceptible to currently used first- and second-line tuberculosis drugs, indicating a lack of cross-resistance. Importantly, an indoleamide derivative exhibits dose-dependent antimycobacterial activity when orally administered to M. tuberculosis-infected mice. The bioavailability of the indoleamides, combined with their ability to kill tubercle bacilli, indicates great potential for translational developments of this structure class for the treatment of drug-resistant tuberculosis.
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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.