Evidence map›Paper›PMID 34592052›Full record

ArticleChemMedChem2021

4-Sulfamoylphenylalkylamides as Inhibitors of Carbonic Anhydrases Expressed in Vibrio cholerae.

Francesca Mancuso, Laura De Luca, Federica Bucolo, Milan Vrabel, Andrea Angeli, Clemente Capasso, Claudiu T Supuran, Rosaria Gitto

Open access · hybridAbstract read
In one paragraph

Article in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.6field-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

4 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Benzenesulfonamide derivatives asJournal of enzyme inhibition and medicinal chemistry · 2023
    Article
  3. Article
  4. 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

8 authors at 4 institutions in 2 countries.

Francesca MancusoCHIBIOFARAM Department, University of Messina, Viale Stagno D'Alcontres, 98166, Messina, Italy.
Laura De LucaCHIBIOFARAM Department, University of Messina, Viale Stagno D'Alcontres, 98166, Messina, Italy.ORCID 0000-0003-0614-5713
Federica BucoloCHIBIOFARAM Department, University of Messina, Viale Stagno D'Alcontres, 98166, Messina, Italy.
Milan VrabelInstitute of Organic Chemistry and Biochemistry (IOCB), Czech Academy of Sciences, Flemingovo nám. 2, 16000, Prague, Czech Republic.
Andrea AngeliNEUROFARBA Department, University of Florence, Via U. Schiff 6, 50019, Florence, Italy.ORCID 0000-0002-1470-7192
Clemente CapassoInstitute of Biosciences and Bioresources, CNR, Via Castellino 111, 80131, Napoli, Italy.
Claudiu T SupuranNEUROFARBA Department, University of Florence, Via U. Schiff 6, 50019, Florence, Italy.ORCID 0000-0003-4262-0323
Rosaria GittoCHIBIOFARAM Department, University of Messina, Viale Stagno D'Alcontres, 98166, Messina, Italy.ORCID 0000-0003-0002-2253
University of Messina · ITUniversity of Florence · ITCzech Academy of Sciences, Institute of Organic Chemistry and Biochemistry · CZInstitute of Biosciences and Bioresources · IT

Funding

Academy of Sciences of the Czech Republic 61388963Italian Ministry of Education, University and Research FISR2019_04819Italian Ministry of Education, University and Research PRIN 201744BN5T
6 · The paper itself

Abstract

A current issue of antimicrobial therapy is the resistance to treatment with worldwide consequences. Thus, the identification of innovative targets is an intriguing challenge in the drug and development process aimed at newer antimicrobial agents. The state-of-art of anticholera therapy might comprise the reduction of the expression of cholera toxin, which could be reached through the inhibition of carbonic anhydrases expressed in Vibrio cholerae (VchCAα, VchCAβ, and VchCAγ). Therefore, we focused our interest on the exploitation of sulfonamides as VchCA inhibitors. We planned to design and synthesize new benzenesulfonamides based on our knowledge of the VchCA catalytic site. The synthesized compounds were tested thus collecting useful SAR information. From our investigation, we identified new potent VchCA inhibitors, some of them displayed high affinity toward VchCAγ class, for which few inhibitors are currently reported in literature. The best interesting VchCAγ inhibitor (S)-N-(1-oxo-1-((4-sulfamoylbenzyl)amino)propan-2-yl)furan-2-carboxamide (40) resulted more active and selective inhibitor when compared with acetazolamide (AAZ) as well as previously reported VchCA inhibitors.

Indexed as

BenzenesulfonamidesCarbonic Anhydrase InhibitorsCarbonic AnhydrasesDose-Response Relationship, DrugHumansModels, MolecularMolecular StructureStructure-Activity RelationshipSulfonamidesVibrio choleraeBenzenesulfonamidesCarbonic Anhydrase InhibitorsCarbonic AnhydrasesSulfonamidesBacterial carbonic anhydrasesDrug DiscoveryEnzymes InhibitorsSulfonamidesVibrio cholerae

Identifiers

PMID34592052
PMCPMC9298201
OpenAlexW3202405004

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.