Evidence map›Paper›PMID 35807514›Full record

ArticleMolecules (Basel, Switzerland)2022

Assessing the Role of a Malonamide Linker in the Design of Potent Dual Inhibitors of Factor Xa and Cholinesterases.

Rosa Purgatorio, Nicola Gambacorta, Francesco Samarelli, Gianfranco Lopopolo, Modesto de Candia, Marco Catto, Orazio Nicolotti, Cosimo D Altomare

Abstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Investigation on NovelMolecules (Basel, Switzerland) · 2023
    Article
  2. 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

8 authors.

Rosa PurgatorioDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0003-1002-5087
Nicola GambacortaDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0003-1965-1519
Francesco SamarelliDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-6753-3528
Gianfranco LopopoloDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.
Modesto de CandiaDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-4570-1981
Marco CattoDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-8411-304X
Orazio NicolottiDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0001-6533-5539
Cosimo D AltomareDepartment of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.ORCID 0000-0001-5016-5805

Funding

Ministry of Education, Universities and Research PRIN, Grant 201744BN5T_004
6 · The paper itself

Abstract

The rational discovery of new peptidomimetic inhibitors of the coagulation factor Xa (fXa) could help set more effective therapeutic options (to prevent atrial fibrillation). In this respect, we explored the conformational impact on the enzyme inhibition potency of the malonamide bridge, compared to the glycinamide one, as a linker connecting the P1 benzamidine anchoring moiety to the P4 aryl group of novel selective fXa inhibitors. We carried out structure-activity relationship (SAR) studies aimed at investigating

Indexed as

BenzamidinesCholinesterase InhibitorsFactor Xa InhibitorsMalonatesAcetylcholinesteraseButyrylcholinesteraseDrug DesignFactor XaFibrinolytic AgentsGlycineMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipAcetylcholinesteraseBenzamidinesButyrylcholinesteraseCholinesterase InhibitorsFactor XaFactor Xa InhibitorsFibrinolytic AgentsGlycineglycine amidemalonamideMalonatesacetylcholinesteraseAlzheimer’s diseaseantithrombotic agentsbutyrylcholinesterasefXa inhibitorsN,N′-malonamidesthrombin inhibitors

Identifiers

PMID35807514
PMCPMC9268553

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.