Evidence map›Paper›PMID 29657102›Full record

ArticleBioorganic & medicinal chemistry letters2018

Agonists of the γ-aminobutyric acid type B (GABA

Munia F Sowaileh, Amy E Salyer, Kuldeep K Roy, Jinu P John, James R Woods, Robert J Doerksen, Gregory H Hockerman, David A Colby

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 39% 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

5 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. Synthesis of α,α-Difluoro-β-amino Ketones fromThe Journal of organic chemistry · 2024
    Article
  3. GABACurrent topics in behavioral neurosciences · 2022
    Review
  4. Article
  5. The GABAMolecules (Basel, Switzerland) · 2020
    Review
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 at 2 institutions in 1 country.

Munia F SowailehDepartment of BioMolecular Sciences, University of Mississippi, University, MS 38677, United States.
Amy E SalyerDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, United States.
Kuldeep K RoyDepartment of BioMolecular Sciences, University of Mississippi, University, MS 38677, United States.
Jinu P JohnDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, United States.
James R WoodsDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, United States.
Robert J DoerksenDepartment of BioMolecular Sciences, University of Mississippi, University, MS 38677, United States.
Gregory H HockermanDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, United States.
David A ColbyDepartment of BioMolecular Sciences, University of Mississippi, University, MS 38677, United States. Electronic address: dacolby@olemiss.edu.
Purdue University West Lafayette · USUniversity of Mississippi · US

Funding

Center of Research Excellence in Natural Products Neuroscience (CORE-NPN)P20GM104932 · NIGMS · UNIVERSITY OF MISSISSIPPI · PI MAJUMDAR, SOUMYAJIT · 2012 to 2016
$10.0M
NIGMS NIH HHS P20 GM104932NIMH NIH HHS HHSN271201300017C
6 · The paper itself

Abstract

β-Hydroxy difluoromethyl ketones represent the newest class of agonists of the GABA-B receptor, and they are structurally distinct from all other known agonists at this receptor because they do not display the carboxylic acid or amino group of γ-aminobutyric acid (GABA). In this report, the design, synthesis, and biological evaluation of additional analogues of β-hydroxy difluoromethyl ketones characterized the critical nature of the substituted aromatic group on the lead compound. The importance of these new data is interpreted by docking studies using the X-ray structure of the GABA-B receptor. Moreover, we also report that the synthesis and biological evaluation of β-amino difluoromethyl ketones provided the most potent compound across these two series.

Indexed as

Binding SitesGABA-B Receptor AgonistsHEK293 CellsHumansKetonesMolecular Docking SimulationPropylaminesReceptors, GABA-BStereoisomerismStructure-Activity RelationshipGABA-B Receptor AgonistsKetonesPropylaminesReceptors, GABA-BAgonistFluorineGABA-BGABA receptorGamma-aminobutyric acid

Identifiers

PMID29657102
PMCPMC6152937
OpenAlexW2796340923

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.