ArticleThe Journal of antimicrobial chemotherapy2011
Interaction of N-methyl-2-alkenyl-4-quinolones with ATP-dependent MurE ligase of Mycobacterium tuberculosis: antibacterial activity, molecular docking and inhibition kinetics.
Article in The Journal of antimicrobial chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 43 citations in OpenAlex.
- The fall of the mycobacterial cell wall: interrogating peptidoglycan synthesis for novel anti-TB agents.PeerJ · 2024Review
- Anti-Tuberculosis Mur Inhibitors: Structural Insights and the Way Ahead for Development of Novel Agents.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Biosynthesis Investigations of Terpenoid, Alkaloid, and Flavonoid Antimicrobial Agents Derived from Medicinal Plants.Antibiotics (Basel, Switzerland) · 2022Review
- OvercomingActa pharmaceutica Sinica. B · 2022Review
- Spectroscopic analysis of 2-(5-mercapto-1,3,4-oxadiazol-2-yl)-6-methylquinolin-4-ol binding to blood plasma albumin.Monatshefte fur chemie · 2022Article
- Characterization of the MurT/GatD complex inJAC-antimicrobial resistance · 2021Article
- Naturally-Occurring Alkaloids of Plant Origin as Potential Antimicrobials against Antibiotic-Resistant Infections.Molecules (Basel, Switzerland) · 2020Review
- Synthesis and Antimicrobial Activity of Novel 4-Hydroxy-2-quinolone Analogs.Molecules (Basel, Switzerland) · 2020Article
- Cell wall peptidoglycan in Mycobacterium tuberculosis: An Achilles' heel for the TB-causing pathogen.FEMS microbiology reviews · 2019Review
- Article
- Docking-based virtual screening of known drugs against murE of Mycobacterium tuberculosis towards repurposing for TB.Bioinformation · 2016Article
- Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase.The Journal of antimicrobial chemotherapy · 2015Article
- Structure based virtual screening to identify inhibitors against MurE Enzyme of Mycobacterium tuberculosis using AutoDock Vina.Bioinformation · 2014Article
- Mycobacterium tuberculosis... Can we beat it? Report from a Euroscicon conference 2013.Virulence · 2013Article
- Progress in targeting cell envelope biogenesis in Mycobacterium tuberculosis.Future microbiology · 2013Review
- Characterisation of ATP-dependent Mur ligases involved in the biogenesis of cell wall peptidoglycan in Mycobacterium tuberculosis.PloS one · 2013Article
- Synthesis and antibacterial evaluation of a new series of N-Alkyl-2-alkynyl/(E)-alkenyl-4-(1H)-quinolones.Molecules (Basel, Switzerland) · 2012Article
- The cell envelope glycoconjugates of Mycobacterium tuberculosis.Critical reviews in biochemistry and molecular biologyReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors at 5 institutions in 2 countries.
Funding
Abstract
objectivesThe aim of this study was to comprehensively evaluate the antibacterial activity and MurE inhibition of a set of N-methyl-2-alkenyl-4-quinolones found to inhibit the growth of fast-growing mycobacteria.
methodsUsing the spot culture growth inhibition assay, MICs were determined for Mycobacterium tuberculosis H(37)Rv, Mycobacterium bovis BCG and Mycobacterium smegmatis mc(2)155. MICs were determined for Mycobacterium fortuitum, Mycobacterium phlei, methicillin-resistant Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa using microplate dilution assays. Inhibition of M. tuberculosis MurE ligase activity was determined both by colorimetric and HPLC methods. Computational modelling and binding prediction of the quinolones in the MurE structure was performed using Glide. Kinetic experiments were conducted for understanding possible competitive relations of the quinolones with the endogenous substrates of MurE ligase.
resultsThe novel synthetic N-methyl-2-alkenyl-4-quinolones were found to be growth inhibitors of M. tuberculosis and rapid-growing mycobacteria as well as methicillin-resistant S. aureus, while showing no inhibition for E. coli and P. aeruginosa. The quinolones were found to be inhibitory to MurE ligase of M. tuberculosis in the micromolar range (IC(50) ∼40-200 μM) when assayed either spectroscopically or by HPLC. Computational docking of the quinolones on the published M. tuberculosis MurE crystal structure suggested that the uracil recognition site is a probable binding site for the quinolones.
conclusionsN-methyl-2-alkenyl-4-quinolones are inhibitors of mycobacterial and staphylococcal growth, and show MurE ligase inhibition. Therefore, they are considered as a starting point for the development of increased affinity MurE activity disruptors.
Indexed as
Identifiers
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.