Evidence map›Paper›PMID 27859446›Full record

ArticleDrug development research2017

Synthesis of Five- and Six-Membered N-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists.

Claudia Vergelli, Igor A Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N Kirpotina, Richard D Ye and 1 more

Open access · greenAbstract read
In one paragraph

Article in Drug development research, 2017. 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
0.2field-weighted citation impact, top 34% 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, 13 citations in OpenAlex.

  1. Review
  2. Article
  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

11 authors at 4 institutions in 4 countries.

Claudia VergelliDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Igor A SchepetkinDepartment of Microbiology and Immunology, Montana State University, Bozeman, Montana 59717.
Giovanna CicianiDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Agostino CilibrizziDepartment of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ, United Kingdom.
Letizia CrocettiDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Maria Paola GiovannoniDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Gabriella GuerriniDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Antonella IacovoneDepartment of NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto, Fiorentino, 50019, Italy.
Liliya N KirpotinaDepartment of Microbiology and Immunology, Montana State University, Bozeman, Montana 59717.
Richard D YeInstitute of Chinese Medical Sciences, University of Macau, Macau, China.
Mark T QuinnDepartment of Microbiology and Immunology, Montana State University, Bozeman, Montana 59717.
University of Florence · ITMontana State University · USImperial College London · GBUniversity of Macau · MO

Funding

Pilot Grants ProgramP30GM110732 · NIGMS · MONTANA STATE UNIVERSITY - BOZEMAN · PI QUINN, MARK T · 2014 to 2018
$5.4M
MOLECULAR MECHANISMS OF LEUKOCYTE ACTIVATIONR01AI033503 · NIAID · UNIVERSITY OF ILLINOIS AT CHICAGO · PI YE, RICHARD D · 1993 to 2014
$4.5M
Molecular Mechanisms of Leukocyte ActivationR56AI033503 · NIAID · UNIVERSITY OF ILLINOIS AT CHICAGO · PI YE, RICHARD D · 2009 to 2009
$393k
NIAID NIH HHS R01 AI033503NIAID NIH HHS R56 AI033503NIGMS NIH HHS P30 GM110732
6 · The paper itself

Abstract

Preclinical Research Formyl peptide receptors (FPRs) are G-protein-coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2, and FPR3). FPR2 appears to be directly involved in the resolution of inflammation, an active process carried out by specific pro-resolving mediators that modulate specific receptors. Previously, we identified 2-arylacetamido pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of mixed-agonists for the three isoforms. Here, we report a new series of 2-arylacetamido pyridazinones substituted at position 5 and their development as FPR agonists. We also synthesized a new series of 2-oxothiazolones bearing a 4-bromophenylacetamido fragment, which was fundamental for activity in the pyridazinone series. The compounds of most interest were 4a, a potent, mixed FPR agonist recognized by all three isotypes (FPR1 EC

Indexed as

AnimalsCells, CulturedHeterocyclic CompoundsHumansMiceModels, MolecularReceptors, Formyl PeptideStructure-Activity RelationshipHeterocyclic CompoundsReceptors, Formyl PeptideagonistCa2+ fluxformyl peptide receptorneutrophilpyridazin-3(2H)-one

Identifiers

PMID27859446
PMCPMC5299035
OpenAlexW2555135784

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.