Evidence map›Paper›PMID 33218895›Full record

ArticleBioorganic & medicinal chemistry2021

Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.

Niccolò Cantini, Andrei I Khlebnikov, Letizia Crocetti, Igor A Schepetkin, Giuseppe Floresta, Gabriella Guerrini, Claudia Vergelli, Gianluca Bartolucci, Mark T Quinn, Maria Paola Giovannoni

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

Article in Bioorganic & medicinal chemistry, 2021. 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
0.7field-weighted citation impact, top 35% 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

5 citing papers in PubMed, 16 citations in OpenAlex.

  1. Review
  2. Target neutrophil heterogeneity and plasticity in cancer.Journal of hematology & oncology · 2025
    Review
  3. Article
  4. Article
  5. 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 4 institutions in 4 countries.

Niccolò CantiniNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Andrei I KhlebnikovNational Research Tomsk Polytechnic University, Tomsk 634050, Russia; Faculty of Chemistry, Tomsk State University, Tomsk 634050, Russia.
Letizia CrocettiNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy. Electronic address: letizia.crocetti@unifi.it.
Igor A SchepetkinDepartment of Microbiology and Immunology, Montana State University, Bozeman, MT, USA.
Giuseppe FlorestaInstitute of Pharmaceutical Science, King's College London, Stamford Street, London SE1 9NH, UK.
Gabriella GuerriniNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Claudia VergelliNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Gianluca BartolucciNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
Mark T QuinnDepartment of Microbiology and Immunology, Montana State University, Bozeman, MT, USA.
Maria Paola GiovannoniNEUROFARBA, Pharmaceutical and Nutraceutical Section, University of Florence, Sesto Fiorentino, Italy.
University of Florence · ITMontana State University · USKing's College London · GBNational Research Tomsk State University · RU

Funding

Research Core (Developmental Research Project Program)P20GM103474 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI Ann Therese Bertagnolli · 2012 to 2026
$60.0M
Tracking and Evaluation CoreU54GM115371 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI QUINN, MARK T, RASMUS, STACY M. · 2016 to 2020
$20.9M
Pilot Grants ProgramP30GM110732 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI QUINN, MARK T · 2014 to 2018
$5.4M
NIGMS NIH HHS P20 GM103474NIGMS NIH HHS P30 GM110732NIGMS NIH HHS U54 GM115371
6 · The paper itself

Abstract

Human neutrophil elastase (HNE) is a potent protease that plays an important physiological role in many processes but is also involved in a variety of pathologies that affect the pulmonary system. Thus, compounds able to inhibit HNE proteolytic activity could represent effective therapeutics. We present here a new series of pyrazolopyridine and pyrrolopyridine derivatives as HNE inhibitors designed as modifications of our previously synthesized indazoles and indoles in order to evaluate effects of the change in position of the nitrogen and/or the insertion of an additional nitrogen in the scaffolds on biological activity and chemical stability. We obtained potent HNE inhibitors with IC

Indexed as

Drug DevelopmentDensity Functional TheoryDose-Response Relationship, DrugHeterocyclic CompoundsHumansLeukocyte ElastaseModels, MolecularMolecular StructurePyridinesPyrrolesSerine Proteinase InhibitorsStructure-Activity RelationshipELANE protein, humanHeterocyclic CompoundsLeukocyte ElastasePyridinesPyrrolesSerine Proteinase InhibitorsADMETHuman neutrophil elastaseInhibitorsMolecular dockingNitrogen heterocycleStability

Identifiers

PMID33218895
PMCPMC8848500
OpenAlexW3097319807

What Socratic holds

Textmetadata
LicenceTDM
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 Socratic graph.