ArticleACS infectious diseases2016
Diphenylether-Modified 1,2-Diamines with Improved Drug Properties for Development against Mycobacterium tuberculosis.
Article in ACS infectious diseases, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 43 citations in OpenAlex.
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- Targeting the Heart of Mycobacterium: Advances in Anti-Tubercular Agents Disrupting Cell Wall Biosynthesis.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Structural modeling and characterization of the Mycobacterium tuberculosis MmpL3 C-terminal domain.FEBS letters · 2024Article
- TheMicrobiology spectrum · 2024Article
- Tackling Nontuberculous Mycobacteria by Repurposable Drugs and Potential Leads from Natural Products.Current topics in medicinal chemistry · 2024Review
- TargetingRSC medicinal chemistry · 2023Review
- 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
- A Hydrazine-Hydrazone Adamantine Compound Shows Antimycobacterial Activity and Is a Probable Inhibitor of MmpL3.Molecules (Basel, Switzerland) · 2022Article
- Proton transfer activity of the reconstitutedProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Cryo-EM structure and resistance landscape of M. tuberculosis MmpL3: An emergent therapeutic target.Structure (London, England : 1993) · 2021Article
- Structural and Functional Diversity of Resistance-Nodulation-Cell Division Transporters.Chemical reviews · 2021Review
- In Silico Screening of the DrugBank Database to Search for Possible Drugs against SARS-CoV-2.Molecules (Basel, Switzerland) · 2021Article
- Modulation of the M. tuberculosis cell envelope between replicating and non-replicating persistent bacteria.Tuberculosis (Edinburgh, Scotland) · 2020Review
- Multiple Mutations in Mycobacterium tuberculosis MmpL3 Increase Resistance to MmpL3 Inhibitors.mSphere · 2020Article
- Triclosan depletes the membrane potential in Pseudomonas aeruginosa biofilms inhibiting aminoglycoside induced adaptive resistance.PLoS pathogens · 2020Article
- Targeting MmpL3 for anti-tuberculosis drug development.Biochemical Society transactions · 2020Review
- Fluorescein Derivatives as Antibacterial Agents Acting via Membrane Depolarization.Biomolecules · 2020Article
- A piperidinol-containing molecule is active againstThe Journal of biological chemistry · 2019Article
- Identification of New MmpL3 Inhibitors by Untargeted and Targeted Mutant Screens Defines MmpL3 Domains with Differential Resistance.Antimicrobial agents and chemotherapy · 2019Article
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Authors and funding
14 authors at 2 institutions in 1 country.
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Abstract
New treatments for tuberculosis infection are critical to combat the emergence of multidrug- and extensively drug-resistant Mycobacterium tuberculosis (Mtb). We report the characterization of a diphenylether-modified adamantyl 1,2-diamine that we refer to as TBL-140, which has a minimal inhibitory concentration (MIC99) of 1.2 μg/mL. TBL-140 is effective against drug-resistant Mtb and nonreplicating bacteria. In addition, TBL-140 eliminates expansion of Mtb in cell culture infection assays at its MIC. To define the mechanism of action of this compound, we performed a spontaneous mutant screen and biochemical assays. We determined that TBL-140 treatment affects the proton motive force (PMF) by perturbing the transmembrane potential (ΔΨ), consistent with a target in the electron transport chain (ETC). As a result, treated bacteria have reduced intracellular ATP levels. We show that TBL-140 exhibits greater metabolic stability than SQ109, a structurally similar compound in clinical trials for treatment of MDR-TB infections. Combined, these results suggest that TBL-140 should be investigated further to assess its potential as an improved therapeutic lead against Mtb.
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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.