Evidence map›Paper›PMID 36615267›Full record

ArticleMolecules (Basel, Switzerland)2022

Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca

Rim Malek, Alexey Simakov, Audrey Davis, Maciej Maj, Paul J Bernard, Artur Wnorowski, Helene Martin, José Marco-Contelles, Fakher Chabchoub, Patrick Dallemagne and 3 more

Open access · goldAbstract 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 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.9field-weighted citation impact, top 15% of its field
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

4 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
  2. Review
  3. Recent Advances in the Search for Effective Anti-Alzheimer's Drugs.International journal of molecular sciences · 2024
    Review
  4. 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

13 authors at 5 institutions in 4 countries.

Rim MalekLaboratoire LINC UR 481, Pôle de Chimie Médicinale, University Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
Alexey SimakovPEPITE EA4267, University Franche-Comté, F-25000 Besançon, France.ORCID 0000-0002-3076-0030
Audrey DavisCentre d'Etudes et de Recherche sur le Médicament de Normandie, Normandie University, Unicaen, CERMN, 14000 Caen, France.ORCID 0000-0002-0157-2380
Maciej MajDepartment of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
Paul J BernardLaboratoire LINC UR 481, Pôle de Chimie Médicinale, University Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
Artur WnorowskiDepartment of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.ORCID 0000-0002-2258-4225
Helene MartinPEPITE EA4267, University Franche-Comté, F-25000 Besançon, France.ORCID 0000-0001-8318-3858
José Marco-ContellesLaboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006 Madrid, Spain.
Fakher ChabchoubLaboratory of Applied Chemistry: Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, Sfax 3000, Tunisia.
Patrick DallemagneCentre d'Etudes et de Recherche sur le Médicament de Normandie, Normandie University, Unicaen, CERMN, 14000 Caen, France.ORCID 0000-0002-4845-615X
Christophe RochaisCentre d'Etudes et de Recherche sur le Médicament de Normandie, Normandie University, Unicaen, CERMN, 14000 Caen, France.ORCID 0000-0001-7996-2082
Krzysztof JozwiakDepartment of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.ORCID 0000-0001-6018-5092
Lhassane IsmailiLaboratoire LINC UR 481, Pôle de Chimie Médicinale, University Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.ORCID 0000-0002-6013-3150
Université de franche-comté · FRMedical University of Lublin · PLNormandie Université · FRUniversity of Sfax · TNInstituto de Química Orgánica General · ES

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Novel multitarget-directed ligands BIGI 4a-d and BIGI 5a-d were designed and synthesized with a simple and cost-efficient procedure via a one-pot three-component Biginelli reaction targeting acetyl-/butyrylcholinesterases inhibition, calcium channel antagonism, and antioxidant ability. Among these multitarget-directed ligands, BIGI 4b, BIGI 4d, and BIGI 5b were identified as promising new hit compounds showing in vitro balanced activities toward the recognized AD targets. In addition, these compounds showed suitable physicochemical properties and a good druglikeness score predicted by Data Warrior software.

Indexed as

Alzheimer DiseaseAntioxidantsCalcium Channel BlockersCholinesterase InhibitorsMolecular Targeted TherapyNF-E2-Related Factor 2HumansLigandsStructure-Activity RelationshipAntioxidantsCalcium Channel BlockersCholinesterase InhibitorsLigandsNF-E2-Related Factor 2Biginelli reactioncalcium channel antagonismmultitarget-directed ligandsNrf2

Identifiers

PMID36615267
PMCPMC9822022
OpenAlexW4312073618

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

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.