Evidence map›Paper›PMID 29256599›Full record

ArticleJournal of medicinal chemistry2018

7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.

Eric Goffin, Thomas Drapier, Anja Probst Larsen, Pierre Geubelle, Christopher P Ptak, Saara Laulumaa, Karoline Rovinskaja, Julie Gilissen, Pascal de Tullio, Lars Olsen and 6 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.7field-weighted citation impact, top 16% 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

10 citing papers in PubMed, 45 citations in OpenAlex.

  1. Review
  2. 5-Nitroisoxazoles inInternational journal of molecular sciences · 2023
    Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. Article
  9. Pharmmaker: Pharmacophore modeling and hit identification based on druggability simulations.Protein science : a publication of the Protein Society · 2020
    Article
  10. 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

16 authors at 3 institutions in 3 countries.

Eric GoffinLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Thomas DrapierLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Anja Probst LarsenBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Pierre GeubelleLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Christopher P PtakDepartment of Molecular Medicine, Cornell University , Ithaca, New York 14850, United States.ORCID 0000-0003-2752-0367
Saara LaulumaaBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Karoline RovinskajaBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Julie GilissenLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Pascal de TullioLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Lars OlsenBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.ORCID 0000-0002-7607-7130
Karla FrydenvangBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Bernard PirotteLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Julien HansonLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.
Robert E OswaldDepartment of Molecular Medicine, Cornell University , Ithaca, New York 14850, United States.
Jette Sandholm KastrupBiostructural Research, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.ORCID 0000-0003-2654-1510
Pierre FrancotteLaboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.ORCID 0000-0001-9252-7798
University of Liège · BEUniversity of Copenhagen · DKCornell University · US

Funding

Overall (pp. 40-62)P41GM103485 · NIGMS · CORNELL UNIVERSITY · PI CERIONE, RICHARD A. · 2012 to 2018
$15.5M
Dynamic properties of a glutamate binding domainR01GM068935 · NIGMS · CORNELL UNIVERSITY ITHACA · PI OSWALD, ROBERT E · 2005 to 2018
$3.4M
Structure, Activation, and Modulation of AMPA/Glutamate ReceptorsR01NS085239 · NINDS · CORNELL UNIVERSITY · PI OSWALD, ROBERT E · 2014 to 2017
$1.4M
Structure, function and dynamics of a glutamate receptorR01NS049223 · NINDS · CORNELL UNIVERSITY · PI OSWALD, ROBERT E · 2006 to 2009
$1.3M
NIGMS NIH HHS P41 GM103485NIGMS NIH HHS R01 GM068935NINDS NIH HHS R01 NS049223NINDS NIH HHS R01 NS085239
6 · The paper itself

Abstract

We report here the synthesis of 7-phenoxy-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides and their evaluation as AMPA receptor positive allosteric modulators (AMPApams). The impact of substitution on the phenoxy ring and on the nitrogen atom at the 4-position was examined. At GluA2(Q) expressed in HEK293 cells (calcium flux experiment), the most potent compound was 11m (4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, EC

Indexed as

Allosteric RegulationBenzothiadiazinesDrug DesignHEK293 CellsHumansReceptors, AMPABenzothiadiazinesReceptors, AMPA

Identifiers

PMID29256599
PMCPMC6052356
OpenAlexW2779847048

What OpenQuestion holds

Textmetadata
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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.