Evidence map›Paper›PMID 36124840›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2022

Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit.

Lisa Vieider, Eva Zoeller, Erik Romp, Martin Schoenthaler, Victor Hernández-Olmos, Veronika Temml, Thomas Hasenoehrl, Daniela Schuster, Oliver Werz, Ulrike Garscha and 1 more

Abstract read
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In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

11 authors.

Lisa VieiderDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Eva ZoellerDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Erik RompDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Jena, Jena, Germany.
Martin SchoenthalerDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Victor Hernández-OlmosBranch for Translation Medicine and Pharmacology TMP, Frauenhofer Institute for Molecular Biology and Applied Ecology IME, Frankfurt am Main, Germany.
Veronika TemmlDepartment of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Paracelsus Medical University Salzburg, Salzburg, Austria.ORCID 0000-0001-7662-9882
Thomas HasenoehrlDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Daniela SchusterDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.ORCID 0000-0002-9933-8938
Oliver WerzDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Jena, Jena, Germany.
Ulrike GarschaDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Greifswald, Greifswald, Germany.
Barbara MatuszczakDepartment of Pharmaceutical Chemistry, Center for Chemistry and Biomedicine, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.ORCID 0000-0002-4507-8739

Funding

Austrian Science Fund FWF T 942
6 · The paper itself

Abstract

A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH and FLAP. Molecular modelling tools were applied to analyse structure-activity relationships (SAR) on both targets and to predict solubility and gastrointestinal (GI) absorption. The most promising dual inhibitors of these series are

Indexed as

BenzimidazolesEpoxide Hydrolases5-Lipoxygenase-Activating ProteinsEnzyme InhibitorsLipoxygenase InhibitorsStructure-Activity Relationship5-Lipoxygenase-Activating ProteinsBenzimidazolesEnzyme InhibitorsEpoxide HydrolasesLipoxygenase Inhibitors5-lipoxygenase activating protein (FLAP)benzimidazolesDiflapolinsolubility and GI absorption predictionsoluble epoxide hydrolase (sEH)

Identifiers

PMID36124840
PMCPMC9518245

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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.