Evidence map›Paper›PMID 31800122›Full record

ArticleDrug development research2020

New 3-unsubstituted isoxazolones as potent human neutrophil elastase inhibitors: Synthesis and molecular dynamic simulation.

Maria Paola Giovannoni, Letizia Crocetti, Niccolò Cantini, Gabriella Guerrini, Claudia Vergelli, Antonella Iacovone, Elisabetta Teodori, Igor A Schepetkin, Mark T Quinn, Samuele Ciattini and 2 more

Abstract read
In one paragraph

Article in Drug development research, 2020. 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
–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

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Affinity of Antifungal Isoxazolo[3,4-Molecules (Basel, Switzerland) · 2020
    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

12 authors.

Maria Paola GiovannoniNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.ORCID 0000-0003-0310-7850
Letizia CrocettiNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.ORCID 0000-0003-3473-2683
Niccolò CantiniNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Gabriella GuerriniNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.ORCID 0000-0001-6711-7965
Claudia VergelliNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Antonella IacovoneNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Elisabetta TeodoriNeurofarba, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Igor A SchepetkinDepartment of Microbiology and Immunology, Montana State University, Bozeman, Montana.
Mark T QuinnDepartment of Microbiology and Immunology, Montana State University, Bozeman, Montana.
Samuele CiattiniCenter of Structural Crystallography, University of Florence, Sesto Fiorentino, Italy.
Patrizia RossiDepartment of Industrial Engineering, University of Florence, Florence, Italy.
Paola PaoliDepartment of Industrial Engineering, University of Florence, Florence, Italy.

Funding

Pilot Grants ProgramP30GM110732 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI QUINN, MARK T · 2014 to 2018
$5.4M
Montana State University Agricultural Experiment StationNational Institutes of Health IDeA Program COBRE GM110732NIGMS NIH HHS P30 GM110732USDA National Institute of Food and Agriculture Hatch project 1009546
6 · The paper itself

Abstract

Human neutrophil elastase (HNE) is a proteolytic enzyme belonging to the serine protease family and is involved in a variety of pathologies. Thus, compounds able to inhibit HNE represent promising therapeutics for the treatment of inflammatory diseases. Here, we report the further elaboration of our previously reported 3-methylisoxazolone derivatives, synthesizing a new series of 3-nor-derivatives bearing different substituents at the 4-phenyl ring. The most potent compounds 3a, 3g, and 3h, had IC

Indexed as

HumansInhibitory Concentration 50IsoxazolesLeukocyte ElastaseModels, MolecularMolecular Dynamics SimulationProteinase Inhibitory Proteins, SecretoryStructure-Activity RelationshipELANE protein, humanIsoxazolesLeukocyte ElastaseProteinase Inhibitory Proteins, Secretoryhuman neutrophil elastase inhibitorsmolecular and crystal structuresmolecular modeling

Identifiers

PMID31800122
PMCPMC9645382

What OpenQuestion holds

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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.