Evidence map›Paper›PMID 33233618›Full record

ArticleInternational journal of molecular sciences2020

The Search for New Anticonvulsants in a Group of (2,5-Dioxopyrrolidin-1-yl)(phenyl)Acetamides with Hybrid Structure-Synthesis and In Vivo/In Vitro Studies.

Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Rafał M Kamiński, Krzysztof Kamiński

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
0.5field-weighted citation impact, top 36% 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

8 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. Discovery of New 3-(Benzo[Pharmaceuticals (Basel, Switzerland) · 2024
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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

7 authors at 1 institution in 1 country.

Michał AbramDepartment of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.ORCID 0000-0001-9738-3359
Marcin JakubiecDepartment of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.
Anna RapaczDepartment of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.
Szczepan MogilskiDepartment of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.ORCID 0000-0002-3072-8890
Gniewomir LataczDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.ORCID 0000-0001-9247-2598
Rafał M KamińskiDepartment of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.
Krzysztof KamińskiDepartment of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.ORCID 0000-0003-2103-371X
Jagiellonian University · PL

Funding

Narodowe Centrum Nauki UMO-2015/18/E/NZ7/00509
6 · The paper itself

Abstract

Epilepsy belongs to the most common and debilitating neurological disorders with multifactorial pathophysiology and a high level of drug resistance. Therefore, with the aim of searching for new, more effective, and/or safer therapeutics, we discovered a focused series of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant properties. We applied an optimized coupling reaction yielding several hybrid compounds that showed broad-spectrum activity in widely accepted animal seizure models, namely, the maximal electroshock (MES) test and the psychomotor 6 Hz (32 mA) seizure model in mice. The most potent anticonvulsant activity and favorable safety profile was demonstrated for compound

Indexed as

AcetamidesAnalgesicsAnimalsAnticonvulsantsCalcium Channels, L-TypeCapsaicinCytochrome P-450 CYP2C9Cytochrome P-450 CYP2D6Cytochrome P-450 CYP3ADisease Models, AnimalDrug Administration ScheduleElectroshockEpilepsy, Complex PartialFormaldehydeGene Expression RegulationHumansAcetamidesAnalgesicsAnticonvulsantsCACNA1C protein, mouseCalcium Channels, L-TypeCapsaicinCYP2C9 protein, humanCYP3A4 protein, humanCytochrome P-450 CYP2C9Cytochrome P-450 CYP2D6Cytochrome P-450 CYP3AFormaldehydeOxaliplatinpyrrolidine-2,5-dionePyrrolidinesabsorption, distribution, metabolism, excretion, toxicity (ADME-Tox) propertiesanticonvulsant activityantinociceptive activityhybrid moleculesin vitro binding/functional studiespyrrolidine-2,5-dione

Identifiers

PMID33233618
PMCPMC7699745
OpenAlexW3101407850

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.