Evidence map›Paper›PMID 28612630›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2017

Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors.

Claudia Vergelli, Igor A Schepetkin, Letizia Crocetti, Antonella Iacovone, Maria Paola Giovannoni, Gabriella Guerrini, Andrei I Khlebnikov, Samuele Ciattini, Giovanna Ciciani, Mark T Quinn

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2017. 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
2.1field-weighted citation impact, top 13% 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, 30 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Review
  6. Article
  7. Neutrophil Elastase Inhibitors and Chronic Kidney Disease.International journal of biological sciences · 2018
    Review
  8. 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

10 authors at 3 institutions in 3 countries.

Claudia Vergellia NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Igor A Schepetkinb Department of Microbiology and Immunology , Montana State University , Bozeman , MT , USA.
Letizia Crocettia NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Antonella Iacovonea NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Maria Paola Giovannonia NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Gabriella Guerrinia NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Andrei I Khlebnikovc Department of Biotechnology and Organic Chemistry , Tomsk Polytechnic University , Tomsk , Russia.
Samuele Ciattinie Dipartimento di Chimica, Centro di Cristallografia , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Giovanna Ciciania NEUROFARBA, Sezione di Farmaceutica e Nutraceutica , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
Mark T Quinnb Department of Microbiology and Immunology , Montana State University , Bozeman , MT , USA.
University of Florence · ITMontana State University · USTomsk Polytechnic University · RU

Funding

Pilot Grants ProgramP30GM110732 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI QUINN, MARK T · 2014 to 2018
$5.4M
NIGMS NIH HHS P30 GM110732
6 · The paper itself

Abstract

Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure-activity relationship analysis, and biological evaluation of a new series of HNE inhibitors with an isoxazol-5(2H)-one scaffold. The most potent compound (2o) had a good balance between HNE inhibitory activity (IC

Indexed as

Dose-Response Relationship, DrugHumansIsoxazolesLeukocyte ElastaseMolecular StructureSerine Proteinase InhibitorsStructure-Activity RelationshipIsoxazolesLeukocyte ElastaseSerine Proteinase Inhibitorschemical stabilityHNE inhibitorhuman neutrophil elastaseIsoxazol-5(2H)-onemolecular docking

Identifiers

PMID28612630
PMCPMC5927774
OpenAlexW2624871753

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.