Evidence map›Paper›PMID 36080139›Full record

ArticleMolecules (Basel, Switzerland)2022

Synthesis of Sulfonamides Incorporating Piperidinyl-Hydrazidoureido and Piperidinyl-Hydrazidothioureido Moieties and Their Carbonic Anhydrase I, II, IX and XII Inhibitory Activity.

Davide Moi, Alessandro Deplano, Andrea Angeli, Gianfranco Balboni, Claudiu T Supuran, Valentina Onnis

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. 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
0.4field-weighted citation impact, top 41% 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, 5 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

6 authors at 2 institutions in 1 country.

Davide MoiDepartment of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Monserrato University Campus, 09042 Monserrato, Italy.ORCID 0000-0002-2470-9351
Alessandro DeplanoPharmacelera, Torre R, 4a Planta, Despatx A05, Parc Cientific de Barcelona, Baldiri Reixac 8, 08028 Barcelona, Spain.ORCID 0000-0002-8451-5831
Andrea AngeliPolo Scientifico Neurofarba Department, Laboratorio di Chimica Bioinorganica, Università Degli Studi di Firenze, Room 188, Via della Lastruccia 3, Sesto Fiorentino, 50019 Florence, Italy.ORCID 0000-0002-1470-7192
Gianfranco BalboniDepartment of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Monserrato University Campus, 09042 Monserrato, Italy.ORCID 0000-0003-4437-6096
Claudiu T SupuranPolo Scientifico Neurofarba Department, Laboratorio di Chimica Bioinorganica, Università Degli Studi di Firenze, Room 188, Via della Lastruccia 3, Sesto Fiorentino, 50019 Florence, Italy.ORCID 0000-0003-4262-0323
Valentina OnnisDepartment of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Monserrato University Campus, 09042 Monserrato, Italy.ORCID 0000-0002-2438-725X
University of Cagliari · ITUniversity of Florence · IT

Funding

Ministry of Education, Universities and Research PRIN 2017, Prot. No. 2010E84AA4_002
6 · The paper itself

Abstract

Here we report a small library of hydrazinocarbonyl-ureido and thioureido benzenesulfonamide derivatives, designed and synthesized as potent and selective human carbonic anhydrase inhibitors (hCAIs). The synthesized compounds were evaluated against isoforms hCA I, II, IX and XII using acetazolamide (AAZ) as standard inhibitor. Several urea and thiourea derivatives showed inhibitory activity at low nanomolar levels with selectivity against the cytosolic hCA II isoform, as well as the transmembrane, tumor-associated enzymes hCA IX and XII. The thiourea derivatives showed enhanced potency as compared to urea analogues. Additionally, eight compounds

Indexed as

Carbonic Anhydrase ICarbonic AnhydrasesCarbonic Anhydrase InhibitorsCarbonic Anhydrase IXHumansMolecular StructureProtein IsoformsStructure-Activity RelationshipSulfanilamideSulfonamidesThioureaUreaCarbonic Anhydrase ICarbonic Anhydrase InhibitorsCarbonic Anhydrase IXCarbonic AnhydrasesProtein IsoformsSulfanilamideSulfonamidesThioureaUreabenzene sulfonamidescarbonic anhydrase inhibitorshydrazidothioureaureashydrazidoureas

Identifiers

PMID36080139
PMCPMC9457746
OpenAlexW4292860079

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.