Skip to content
DraconiticResearch
Search Sources API
197,788 studies31 sourcesUpdated 35 min ago
Peer-reviewedCC BY-NC-NDACS omega

Synthesis and Antischistosomal Activity Profile of Several Sub-Series of Redox-Active Lead 3‑BenzylmenadionesInvestigations of the Modes of Action in Yeast

  • Jeremy Pecourneau1
  • Jimmy Richard1
  • Brigitte Meunier2
  • Maude Dagenais3
  • Cécile Häberli3
  • David L. Williams4
  • Jennifer Keiser3
  • Elisabeth Davioud-Charvet1
4 affiliations
  1. 1Laboratoire d’Innovation Moléculaire et Applications (LIMA), Team Bio(IN)organic and Medicinal Chemistry , UMR7042 CNRS-Université de Strasbourg-Université Haute-Alsace, European School of Chemistry, Polymers and Materials (ECPM) , 25, rue Becquerel , ,
  2. 2Université Paris-Saclay , CEA, CNRS, Institute for Integrative Biology of the Cell (I2BC) , ,
  3. 3, Kreuzstrasse 2 , ,
  4. 4Department of Microbial Pathogens and Immunity , Rush University Medical Center , 1735 West Harrison Street , , ,
Read full textPDFDOICite

Abstract

Three sub-series of 3-benzylmenadiones were discovered as new antischistosomal agents. The most potent representatives, called schistodiones, exhibited IC50 values <5 μM against larvae and ex vivoSchistosoma mansoni adult worms and moderate activity per os in the S. mansoni-infected mouse model in vivo. We synthesized the putative 3-benzoylmenadione metabolites of the most active compounds and explored the possible mode(s) of action using the yeast model and the recombinant drug target S. mansoni thioredoxin-glutathione reductase. Two drug targets were identified in yeast: the yeast NADH dehydrogenase and Cox15, involved in events responsible for respiratory growth defect in yeast, respectively: (i) the bioreductive activation step producing reactive oxygen species and (ii) the heme a synthase inhibition. These two drug targets are discussed in the context of S.mansoni biology, with S. mansoni thioredoxin–glutathione reductase redox-cycling and a potential source of oxidative stress in the parasite.

Related

  1. Frequency and Laminar Profile of Feature Specific Visual Activity Revealed by Interleaved EEG-fMRI
    Tommy Clausner, José Marques, René Scheeringa +1
    eLifePeer-reviewedCC BY 4.0Full textGeneral biologyHAL
  2. Exploring the Chemical Profile and Biological Activities of Eryngium dichotomum: UHPLC–MS/NMR Characterization, and In Vitro Antioxidant Activity Along with the Antitumor Effect of Falcarinol
    Roufia Mezaache, Habiba Laraoui, Anis Bertella +10
    MoleculesPeer-reviewedCC BY 4.0Full textPlant biologyHAL
  3. Improving the Polyphenol Profile, Antioxidant and Antiglycation Activity of Onion Outer Scales with Chamomile Treatment.
    Valerija Vujčić Bok, Sanja Gagić, Lucija Rubinić +5
    Food technology and biotechnologyPeer-reviewedCC BYFull textPlant biologyEurope PMC
  4. The association between honey consumption amount and physical activity, sleep quality, and Nottingham health profile in young adults.
    Fatih Çakar
    BMC public healthPeer-reviewedCC BY-NC-NDFull textZoology & animal behaviourEurope PMCDOAJ
  5. Design, Synthesis, and Structure–Activity Relationship Studies of Spirotryprostatin A-Inspired Spirooxindole-Diketopiperazine Derivatives with Antifungal Activity
    Murong Zhan, Yangmin Ma, Gege Dang +3
    MoleculesPeer-reviewedCC BY 4.0EcologyCrossref

Cite

BibTeXRIS
BibTeX
@article{pecourneau2026synthesis,
  title = {{Synthesis and Antischistosomal Activity Profile of Several Sub-Series of Redox-Active Lead 3‑BenzylmenadionesInvestigations of the Modes of Action in Yeast}},
  author = {Jeremy Pecourneau and Jimmy Richard and Brigitte Meunier and Maude Dagenais and Cécile Häberli and David L. Williams and Jennifer Keiser and Elisabeth Davioud-Charvet},
  journal = {ACS omega},
  year = {2026},
  month = sep,
  doi = {10.1021/acsomega.6c06911},
  url = {https://europepmc.org/article/PMC/PMC13670326},
  note = {CC BY-NC-ND},
}
RIS
TY  - JOUR
TI  - Synthesis and Antischistosomal Activity Profile of Several Sub-Series of Redox-Active Lead 3‑BenzylmenadionesInvestigations of the Modes of Action in Yeast
AU  - Jeremy Pecourneau
AU  - Jimmy Richard
AU  - Brigitte Meunier
AU  - Maude Dagenais
AU  - Cécile Häberli
AU  - David L. Williams
AU  - Jennifer Keiser
AU  - Elisabeth Davioud-Charvet
PY  - 2026
DA  - 2026/09/29
JO  - ACS omega
DO  - 10.1021/acsomega.6c06911
UR  - https://europepmc.org/article/PMC/PMC13670326
AB  - Three sub-series of 3-benzylmenadiones were discovered as new antischistosomal agents. The most potent representatives, called schistodiones, exhibited IC50 values <5 μM against larvae and ex vivoSchistosoma mansoni adult worms and moderate activity per os in the S. mansoni-infected mouse model in vivo. We synthesized the putative 3-benzoylmenadione metabolites of the most active compounds and explored the possible mode(s) of action using the yeast model and the recombinant drug target S. mansoni thioredoxin-glutathione reductase. Two drug targets were identified in yeast: the yeast NADH dehydrogenase and Cox15, involved in events responsible for respiratory growth defect in yeast, respectively: (i) the bioreductive activation step producing reactive oxygen species and (ii) the heme a synthase inhibition. These two drug targets are discussed in the context of S.mansoni biology, with S. mansoni thioredoxin–glutathione reductase redox-cycling and a potential source of oxidative stress in the parasite.
SN  - 2470-1343
ER  -