Evidence map›Paper›PMID 27134116›Full record

ArticleBioorganic & medicinal chemistry2016

2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists.

Claudia Vergelli, Igor A Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N Kirpotina, Andrei I Khlebnikov and 2 more

Open access · bronzeAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.0field-weighted citation impact, top 22% 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

10 citing papers in PubMed, 24 citations in OpenAlex.

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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

12 authors at 5 institutions in 5 countries.

Claudia VergelliDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Igor A SchepetkinDepartment of Microbiology and Immunology, Montana State University, Bozeman, MT 59717, USA.
Giovanna CicianiDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Agostino CilibrizziDepartment of Chemistry, Imperial College London, South Kensington, London SW7 2AZ, UK.
Letizia CrocettiDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Maria Paola GiovannoniDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy. Electronic address: mariapaola.giovannoni@unifi.it.
Gabriella GuerriniDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Antonella IacovoneDipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Liliya N KirpotinaDepartment of Microbiology and Immunology, Montana State University, Bozeman, MT 59717, USA.
Andrei I KhlebnikovDepartment of Biotechnology and Organic Chemistry, Tomsk Polytechnic University, Tomsk 634050, Russia; Department of Chemistry, Altai State Technical University, Barnaul, Russia.
Richard D YeInstitute of Chinese Medical Sciences, University of Macau, Macau.
Mark T QuinnDepartment of Microbiology and Immunology, Montana State University, Bozeman, MT 59717, USA.
University of Florence · ITMontana State University · USImperial College London · GBTomsk Polytechnic University · RUUniversity 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

N-Formyl peptide receptors (FPRs: FPR1, FPR2, and FPR3) are G protein-coupled receptors that play key roles in modulating immune cells. FPRs represent potentially important therapeutic targets for the development of drugs that could enhance endogenous anti-inflammation systems associated with various pathologies, thereby reducing the progression of inflammatory conditions. Previously, we identified 2-arylacetamide pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of FPR1/FPR2-dual agonists and several mixed-agonists for the three FPR isoforms. Here, we report a new series of 2-arylacetamido-4-aniline pyridazin-3(2H)-ones substituted in position 5 as a further development of these FPR agonists. Chemical manipulation presented in this work resulted in mixed FPR agonists 8a, 13a and 27b, which had EC

Indexed as

AgonistCa(2+) mobilizationFormyl peptide receptor (FPR)NeutrophilPyridazin-3(2H)-one

Identifiers

PMID27134116
PMCPMC5055850
OpenAlexW2324597919

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.