ArticleJournal of medicinal chemistry2018
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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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
29 citing papers in PubMed, 57 citations in OpenAlex.
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- New Triazolopyrimidines with Improved Activity againstACS medicinal chemistry letters · 2025Article
- Deep learning-driven bacterial cytological profiling to determine antimicrobial mechanisms inProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Structural and mechanistic study of a novel inhibitor analogue ofnpj drug discovery · 2025Article
- An open-access dashboard to interrogate the genetic diversity of Mycobacterium tuberculosis clinical isolates.Scientific reports · 2024Article
- Polyketide Synthase 13 (Pks13) Inhibition: A Potential Target for New Class of Anti-tubercular Agents.Current topics in medicinal chemistry · 2024Review
- Benzene Amide Ether Scaffold is Active against Non-replicating and IntracellularACS infectious diseases · 2023Article
- Review
- Molecular Mechanisms of MmpL3 Function and Inhibition.Microbial drug resistance (Larchmont, N.Y.) · 2023Review
- A base-catalyzed approach for the anti-Markovnikov hydration of styrene derivatives.Chemical science · 2022Article
- Targeting the cytochrome bcMolecular diversity · 2022Review
- Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening.Scientific reports · 2022Article
- Prediction of QcrB Inhibition as a Measure of Antitubercular Activity with Machine Learning Protocols.ACS omega · 2022Article
- Triazolopyrimidines Target Aerobic Respiration in Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 2022Article
- A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen).European journal of medicinal chemistry · 2022Article
- Recent Discoveries of Nitrogen-Containing Heterocyclic Compounds as InhA Inhibitors againstInfectious disorders drug targets · 2022Article
- LigTMap: ligand and structure-based target identification and activity prediction for small molecular compounds.Journal of cheminformatics · 2021Article
- Metabolic Versatility ofMetabolites · 2021Review
- Tuberculosis Drug Discovery: A Decade of Hit Assessment for Defined Targets.Frontiers in cellular and infection microbiology · 2021Review
Corrections and comments
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Authors and funding
26 authors at 4 institutions in 3 countries.
Funding
Abstract
With the emergence of multidrug-resistant strains of Mycobacterium tuberculosis there is a pressing need for new oral drugs with novel mechanisms of action. Herein, we describe the identification of a novel morpholino-thiophenes (MOT) series following phenotypic screening of the Eli Lilly corporate library against M. tuberculosis strain H37Rv. The design, synthesis, and structure-activity relationships of a range of analogues around the confirmed actives are described. Optimized leads with potent whole cell activity against H37Rv, no cytotoxicity flags, and in vivo efficacy in an acute murine model of infection are described. Mode-of-action studies suggest that the novel scaffold targets QcrB, a subunit of the menaquinol cytochrome c oxidoreductase, part of the bc1-aa3-type cytochrome c oxidase complex that is responsible for driving oxygen-dependent respiration.
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What OpenQuestion holds
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.