Evidence map›Paper›PMID 42723276›Full record

ArticleChemMedChem2026

Synthesis and Evaluation of Peptoid-Based Compound Libraries as Inhibitors of Parasite Metallo-Aminopeptidases.

Mirta Elisa Aguado, Gerardo M Ojeda-Carralero, Mario Antonio Rodríguez, Isabella Rúa, Heisy Guerra, Edoardo Bailo Hernández, Guglielmo Coppola, Susana Alberti, Ariatne Rodríguez, Maikel Izquierdo and 7 more

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Article in ChemMedChem, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. Article
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

17 authors.

Mirta Elisa AguadoCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.
Gerardo M Ojeda-CarraleroLaboratory of Synthetic and Biomolecular Chemistry, Faculty of Chemistry, University of Havana, Havana, Cuba.ORCID https://orcid.org/0000-0002-9639-7852
Mario Antonio RodríguezCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.ORCID https://orcid.org/0009-0008-0104-7421
Isabella RúaCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.ORCID https://orcid.org/0009-0006-7728-7427
Heisy GuerraCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.
Edoardo Bailo HernándezLaboratory of Synthetic and Biomolecular Chemistry, Faculty of Chemistry, University of Havana, Havana, Cuba.ORCID https://orcid.org/0009-0004-7906-8581
Guglielmo CoppolaLaboratory for Organic and Microwave-assisted Chemistry (LOMAC), Department of Chemistry, Leuven, Belgium.ORCID https://orcid.org/0000-0001-9744-3665
Susana AlbertiCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.
Ariatne RodríguezCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.
Maikel IzquierdoCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.
Christian BetzelInstitute of Biochemistry and Molecular Biology, Laboratory for Structural Biology of Infection and Inflammation, University of Hamburg, Hamburg, Germany.
Filippo PettazziLaboratory for Organic and Microwave-assisted Chemistry (LOMAC), Department of Chemistry, Leuven, Belgium.
Julieta Coro-BermelloLaboratory of Synthetic and Biomolecular Chemistry, Faculty of Chemistry, University of Havana, Havana, Cuba.
Erik V Van der EyckenLaboratory for Organic and Microwave-assisted Chemistry (LOMAC), Department of Chemistry, Leuven, Belgium.
Bernhard WestermannDepartment of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Halle (Saale), Germany.ORCID https://orcid.org/0000-0002-6228-5991
Jorge González-BacerioCenter for Protein Studies, Faculty of Biology, University of Havana, Havana, Cuba.ORCID https://orcid.org/0000-0002-7155-9165
Daniel G RiveraLaboratory of Synthetic and Biomolecular Chemistry, Faculty of Chemistry, University of Havana, Havana, Cuba.ORCID https://orcid.org/0000-0002-5538-1555

Funding

Alexander von Humboldt-StiftungDeutsche Forschungsgemeinschaft 390715994German Academic Exchange Service 57592717VLIRUOS CU2018-TEA458A101
6 · The paper itself

Abstract

Parasitic diseases are a worldwide health and socio-economical problem, especially due to increasing parasite resistance and frequent toxicity of commercial drugs. Parasite metallo-aminopeptidases are potential therapeutic targets, as they perform crucial biological functions during parasite development within the human host. Here, we describe the synthesis and biological evaluation of two libraries consisting of a total of 74 peptoid-based compounds. The synthetic approaches use a multicomponent reaction to install various diversity elements, and in library one, this is followed by subsequent coupling to α-amino acids to create further diversity within a peptoid-peptide hybrid skeleton. The libraries were evaluated against three metallo-aminopeptidases: PfA-M1 from Plasmodium falciparum, TcLAP from Trypanosoma cruzi, and LmLAP from Leishmania major, which allowed the discovery of moderate to potent inhibitors of each enzyme. Molecular docking studies were conducted to help understand the binding mode of the inhibitors with the enzymes, predicting the importance of hydrophobic interactions in the inhibition process.

Indexed as

AminopeptidasesEnzyme InhibitorsPeptoidsPlasmodium falciparumProtease InhibitorsSmall Molecule LibrariesDose-Response Relationship, DrugHumansLeishmania majorMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipTrypanosoma cruziAminopeptidasesEnzyme InhibitorsPeptoidsProtease InhibitorsSmall Molecule LibrariesChagasenzyme inhibitorsleishmaniamalariametallo‐aminopeptidasesmulticomponent reactionspeptoids

Identifiers

PMID42723276
PMCPMC13562828

What OpenQuestion holds

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Registered trials

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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.