Evidence map›Paper›PMID 28097874›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2017

Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B.

Rita Meleddu, Simona Distinto, Roberto Cirilli, Stefano Alcaro, Matilde Yanez, Maria Luisa Sanna, Angela Corona, Claudia Melis, Giulia Bianco, Peter Matyus and 2 more

Abstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. The synthetic and therapeutic expedition of isoxazole and its analogs.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2018
    Review
  7. Review
  8. 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

12 authors.

Rita Meleddua Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Simona Distintoa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Roberto Cirillib Dipartimento del Farmaco , Istituto Superiore di Sanità , Rome , Italy.
Stefano Alcaroc Dipartimento di Scienze della Salute , Università Magna Græcia di Catanzaro , Catanzaro , Italy.
Matilde Yanezd Departamento de Farmacología and Instituto de Farmacia Industrial , Universidad de Santiago de Compostela, Campus Universitario Sur , Santiago de Compostela , Spain.
Maria Luisa Sannaa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Angela Coronaa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Claudia Melisa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Giulia Biancoa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Peter Matyuse Department of Organic Chemistry , Semmelweis University , Budapest , Hungary.
Filippo Cottigliaa Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
Elias Maccionia Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

3,5-Diaryl-4,5-dihydroisoxazoles were synthesized and evaluated as monoamine oxidase (MAO) enzyme inhibitors and iron chelators. All compounds exhibited selective inhibitory activity towards the B isoform of MAO in the nanomolar concentration range. The best performing compound was preliminarily evaluated for its ability to bind iron II and III cations, indicating that neither iron II nor iron III is coordinated. The best compounds racemic mixtures were separated and single enantiomers inhibitory activity evaluated. Furthermore, none of the synthesised compounds exhibited activity towards MAO A. Overall, these data support our hypothesis that 3,5-diaryl-4,5-dihydroisoxazoles are promising scaffolds for the design of neuroprotective agents.

Indexed as

IsoxazolesModels, MolecularMonoamine OxidaseMonoamine Oxidase InhibitorsStructure-Activity RelationshipIsoxazolesMonoamine OxidaseMonoamine Oxidase Inhibitors3,5-diaryl-dihydroisoxazolesMAO B selective inhibitorsneuroprotective agents

Identifiers

PMID28097874
PMCPMC6009968

What OpenQuestion holds

Textmetadata
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.