Evidence map›Paper›PMID 40042998›Full record

ArticleJournal of medicinal chemistry2025

Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor.

Beatrice Noce, Sara Marchese, Marta Massari, Chiara Lambona, Joana Reis, Francesco Fiorentino, Alessia Raucci, Rossella Fioravanti, Mariana Castelôa, Alessandro Mormino and 8 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
  4. Article
  5. Review
  6. Enhancing Selectivity and Potency of SJournal of medicinal chemistry · 2025
    Article
  7. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

18 authors.

Beatrice NoceDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.
Sara MarcheseDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.
Marta MassariDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.
Chiara LambonaDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.ORCID 0000-0002-3415-4126
Joana ReisDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.
Francesco FiorentinoDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.ORCID 0000-0003-3550-1860
Alessia RaucciDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.
Rossella FioravantiDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.
Mariana CastelôaCIQUP-IMS/Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre s/n, Porto 4169-007, Portugal.ORCID 0000-0002-0913-3219
Alessandro MorminoDepartment of Physiology and Pharmacology, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.
Stefano GarofaloDepartment of Physiology and Pharmacology, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.
Cristina LimatolaDepartment of Physiology and Pharmacology, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.ORCID 0000-0001-7504-8197
Lorenzo BasileDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.ORCID 0009-0004-6724-0110
Andrea GottingerDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.
Claudia BindaDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.ORCID 0000-0003-2038-9845
Andrea MatteviDepartment of Biology and Biotechnology Lazzaro Spallanzani, University of Pavia, Via Adolfo Ferrata 9A, Pavia 27100, Italy.ORCID 0000-0002-9523-7128
Antonello MaiDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.ORCID 0000-0001-9176-2382
Sergio ValenteDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, Rome 00185, Italy.ORCID 0000-0002-2241-607X

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

NADPH oxidases (NOXs) are enzymes dedicated to reactive oxygen species (ROS) production and are implicated in cancer, neuroinflammation, and neurodegenerative diseases. VAS2870 is a covalent inhibitor of mainly NOX2 and NOX5. It alkylates a conserved active-site cysteine, blocking productive substrate binding. To enhance potency and selectivity toward NOXs, we conducted some chemical modifications, leading to the discovery of compound

Indexed as

Drug DesignMonoamine Oxidase InhibitorsNADPH Oxidase 2PyrimidinesTriazolesAnimalsCell LineHumansMiceMicrogliaMonoamine OxidaseNADPH OxidasesReactive Oxygen SpeciesStructure-Activity RelationshipMonoamine OxidaseMonoamine Oxidase InhibitorsNADPH Oxidase 2NADPH OxidasesPyrimidinesReactive Oxygen SpeciesTriazoles

Identifiers

PMID40042998
PMCPMC11956017

What OpenQuestion holds

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Registered trials

None linked

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.