Evidence map›Paper›PMID 30362376›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2019

Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [

Jonathan Elie, Johnny Vercouillie, Nicolas Arlicot, Lucas Lemaire, Rudy Bidault, Sylvie Bodard, Christel Hosselet, Jean-Bernard Deloye, Sylvie Chalon, Patrick Emond and 3 more

Abstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing 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

16 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. Article
  5. Review
  6. Design, Synthesis,Anti-cancer agents in medicinal chemistry · 2024
    Article
  7. State of the art procedures towards reactive [EJNMMI radiopharmacy and chemistry · 2023
    Review
  8. Article
  9. Review
  10. Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022
    Review
  11. Review
  12. Article
  13. Article
  14. Article
  15. Synthesis of high-molar-activity [Nature protocols · 2020
    Article
  16. 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.

Jonathan Eliea ICOA, UMR CNRS 7311 , University of Orleans , Orleans , France.
Johnny Vercouillieb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Nicolas Arlicotb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Lucas Lemairea ICOA, UMR CNRS 7311 , University of Orleans , Orleans , France.
Rudy Bidaultb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Sylvie Bodardb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Christel Hosseletb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Jean-Bernard Deloyec CERRP , Centre d'Etude et de Recherche sur les Radiopharmaceutiques , Tours , France.
Sylvie Chalonb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Patrick Emondb UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Denis Guilloteaub UMR 1253, iBrain , Université de Tours, Inserm , Tours , France.
Frédéric Burona ICOA, UMR CNRS 7311 , University of Orleans , Orleans , France.
Sylvain Routiera ICOA, UMR CNRS 7311 , University of Orleans , Orleans , France.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C-H activation were established in the indazole and azaindazole series respectively. In vitro assays were conducted and structural modifications were carried out on these scaffolds to furnish compound 16 which exhibited effective COX-2 inhibitory activity, with IC

Indexed as

Positron-Emission TomographyAnimalsAza CompoundsCyclooxygenase 2Cyclooxygenase 2 InhibitorsDose-Response Relationship, DrugFluorine RadioisotopesIndazolesMolecular StructureRadioactive TracersRadiopharmaceuticalsRatsStructure-Activity RelationshipAza CompoundsCyclooxygenase 2Cyclooxygenase 2 InhibitorsFluorine RadioisotopesIndazolesRadioactive TracersRadiopharmaceuticals(aza)indazolesboronic esterCyclooxygenaseneuroinflammationNSAIDPETradiolabeling

Identifiers

PMID30362376
PMCPMC6211253

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.