Evidence map›Paper›PMID 30108813›Full record

ArticleMedChemComm2017

Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors.

Hui Deng, Tom van der Wel, Richard J B H N van den Berg, Adrianus M C H van den Nieuwendijk, Freek J Janssen, Marc P Baggelaar, Hermen S Overkleeft, Mario van der Stelt

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

Article in MedChemComm, 2017. 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
0.8field-weighted citation impact, top 28% 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, 9 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. ABHD6: Its Place in Endocannabinoid Signaling and Beyond.Trends in pharmacological sciences · 2019
    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 1 institution in 1 country.

Hui DengDepartment of Molecular Physiology , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands . Email: m.van.der.stelt@chem.leidenuniv.nl.ORCID 0000-0003-0899-4188
Tom van der WelDepartment of Molecular Physiology , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands . Email: m.van.der.stelt@chem.leidenuniv.nl.
Richard J B H N van den BergDepartment of Bio-organic Synthesis , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Adrianus M C H van den NieuwendijkDepartment of Bio-organic Synthesis , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Freek J JanssenDepartment of Molecular Physiology , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands . Email: m.van.der.stelt@chem.leidenuniv.nl.
Marc P BaggelaarDepartment of Molecular Physiology , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands . Email: m.van.der.stelt@chem.leidenuniv.nl.
Hermen S OverkleeftDepartment of Bio-organic Synthesis , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Mario van der SteltDepartment of Molecular Physiology , Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands . Email: m.van.der.stelt@chem.leidenuniv.nl.
Leiden University · NL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibitors of diacylglycerol lipases and α,β-hydrolase domain containing protein 6 (ABHD6) are potential leads for the development of therapeutic agents for metabolic and neurodegenerative disorders. Here, we report the enantioselective synthesis and structure activity relationships of triazole ureas featuring chiral, hydroxylated 2-benzylpiperidines as dual inhibitors of DAGLα and ABHD6. The chirality of the carbon bearing the C2 substituent, as well as the position of the hydroxyl (tolerated at C5, but not at C3) has profound influence on the inhibitory activity of both DAGLα and ABHD6, as established using biochemical assays and competitive activity-based protein profiling on mouse brain extracts.

Identifiers

PMID30108813
PMCPMC6071720
OpenAlexW2593072972

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.