ArticleFuture medicinal chemistry2016
Discovery of bicyclic inhibitors against menaquinone biosynthesis.
Article in Future medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed.
- Efficacy and Possible Mechanism(s) of Action of Gallium Tetraphenylporphyrin Nanoparticles against HIV-TB Coinfection in anACS infectious diseases · 2024Article
- Unraveling bacterial stress responses: implications for next-generation antimicrobial solutions.World journal of microbiology & biotechnology · 2024Article
- Advances in regulating vitamin KWorld journal of microbiology & biotechnology · 2023Review
- SAR study of piperidine derivatives as inhibitors of 1,4-dihydroxy-2-naphthoate isoprenyltransferase (MenA) from Mycobacterium tuberculosis.European journal of medicinal chemistry · 2023Article
- Allosteric inhibition ofPhilosophical transactions of the Royal Society of London. Series B, Biological sciences · 2023Article
- New Insights Into the Antibacterial Mechanism of Cryptotanshinone, a Representative Diterpenoid Quinone FromFrontiers in microbiology · 2021Article
- The Role of Metallic Nanoparticles in Inhibition of Mycobacterium Tuberculosis and Enhances Phagosome Maturation into the Infected Macrophage.Oman medical journal · 2020Review
- Novel MenA Inhibitors Are Bactericidal againstAntimicrobial agents and chemotherapy · 2019Article
- Characterization of MenA (isoprenyl diphosphate:1,4-dihydroxy-2-naphthoate isoprenyltransferase) from Mycobacterium tuberculosis.PloS one · 2019Article
- Neuroprotection through flavonoid: Enhancement of the glyoxalase pathway.Redox biology · 2018Review
- Bioenergetics of Mycobacterium: An Emerging Landscape for Drug Discovery.Pathogens (Basel, Switzerland) · 2018Review
- Menaquinone biosynthesis inhibition: a review of advancements toward a new antibiotic mechanism.RSC advances · 2018Review
- A Synthetic Isoprenoid Lipoquinone, Menaquinone-2, Adopts a Folded Conformation in Solution and at a Model Membrane Interface.The Journal of organic chemistry · 2018Article
- Ga(III) Nanoparticles Inhibit Growth of both Mycobacterium tuberculosis and HIV and Release of Interleukin-6 (IL-6) and IL-8 in Coinfected Macrophages.Antimicrobial agents and chemotherapy · 2017Article
- Novel long-chain compounds with both immunomodulatory and MenA inhibitory activities against Staphylococcus aureus and its biofilm.Scientific reports · 2017Article
- Gallium nanoparticles facilitate phagosome maturation and inhibit growth of virulent Mycobacterium tuberculosis in macrophages.PloS one · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors.
Funding
Abstract
introductionMenaquinone is used for transporting electrons and is essential for the aerobic and anaerobic respiratory systems of all pathogens and prokaryotes. Many Gram-positive bacteria use only menaquinone in the electron transport system. Thus, menaquinone biosynthesis is a potential target for the development of inhibitors against bacteria including drug-resistant pathogens.
resultsAfter modeling, synthesis and in vitro testing, we determined that 7-methoxy-2-naphthol-based inhibitors targeted the MenA enzyme of the menaquinone biosynthesis pathway. The developmental compounds 1 and 2 were active against Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus with a minimal inhibitory concentration of 3-5 μg/ml.
conclusionNontraditional bicyclic inhibitors, compounds 1 and 2 could serve as lead compounds for the development of an antimicrobial agent, with activities against M. tuberculosis and methicillin-resistant S. aureus.
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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.