Evidence map›Paper›PMID 31537132›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2019

Novel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies.

Ciro Milite, Giorgio Amendola, Alessio Nocentini, Silvia Bua, Alessandra Cipriano, Elisabetta Barresi, Alessandra Feoli, Ettore Novellino, Federico Da Settimo, Claudiu T Supuran and 3 more

Abstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
–field-weighted citation impact
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

14 citing papers in PubMed.

  1. Review
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  13. Coumarin carbonic anhydrase inhibitors from natural sources.Journal of enzyme inhibition and medicinal chemistry · 2020
    Review
  14. 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

13 authors.

Ciro MiliteDepartment of Pharmacy, Epigenetic Med Chem Lab, University of Salerno , Fisciano (SA) , Italy.ORCID http://orcid.org/0000-0003-1000-1376
Giorgio AmendolaDiSTABiF, Università della Campania Luigi Vanvitelli , Caserta , Italy.ORCID http://orcid.org/0000-0003-4271-5031
Alessio NocentiniNEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.ORCID http://orcid.org/0000-0003-3342-702X
Silvia BuaNEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.ORCID http://orcid.org/0000-0003-0107-2682
Alessandra CiprianoDepartment of Pharmacy, Epigenetic Med Chem Lab, University of Salerno , Fisciano (SA) , Italy.ORCID http://orcid.org/0000-0002-9062-5914
Elisabetta BarresiDepartment of Pharmacy, Universy of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-9814-7195
Alessandra FeoliDepartment of Pharmacy, Epigenetic Med Chem Lab, University of Salerno , Fisciano (SA) , Italy.ORCID http://orcid.org/0000-0002-8960-7858
Ettore NovellinoDepartment of Pharmacy, University Federico II of Naples , Naples , Italy.ORCID http://orcid.org/0000-0002-2181-2142
Federico Da SettimoDepartment of Pharmacy, Universy of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-7897-7917
Claudiu T SupuranNEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.ORCID http://orcid.org/0000-0003-4262-0323
Sabrina CastellanoDepartment of Pharmacy, Epigenetic Med Chem Lab, University of Salerno , Fisciano (SA) , Italy.ORCID http://orcid.org/0000-0002-7449-3704
Sandro CosconatiDiSTABiF, Università della Campania Luigi Vanvitelli , Caserta , Italy.ORCID http://orcid.org/0000-0002-8900-0968
Sabrina TalianiDepartment of Pharmacy, Universy of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0001-8675-939X

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibition of Carbonic Anhydrases (CAs) has been clinically exploited for many decades for a variety of therapeutic applications. Within a research project aimed at developing novel classes of CA inhibitors (CAIs) with a proper selectivity for certain isoforms, a series of derivatives featuring the 2-substituted-benzimidazole-6-sulfonamide scaffold, conceived as frozen analogs of Schiff bases and secondary amines previously reported in the literature as CAIs, were investigated. Enzyme inhibition assays on physiologically relevant human CA I, II, IX and XII isoforms revealed a number of potent CAIs, showing promising selectivity profiles towards the transmembrane tumor-associated CA IX and XII enzymes. Computational studies were attained to clarify the structural determinants behind the activities and selectivity profiles of the novel inhibitors.

Indexed as

AminesBenzimidazolesCarbonic Anhydrase ICarbonic Anhydrase IICarbonic Anhydrase InhibitorsCarbonic AnhydrasesCarrier ProteinsHumansIsoenzymesMolecular Docking SimulationMolecular StructureNerve Tissue ProteinsSchiff BasesStructure-Activity RelationshipSulfonamidesAminesBenzimidazolesCA11 protein, humanCA1 carbonic anhydrase, humanCA2 protein, humanCarbonic Anhydrase ICarbonic Anhydrase IICarbonic Anhydrase InhibitorsCarbonic AnhydrasesCarrier ProteinsIsoenzymesNerve Tissue ProteinsSchiff BasesSulfonamidesbenzimidazole-sulfonamidesCarbonic anhydrase inhibitorsisoform-selective inhibitorsmolecular dockingreduced flexibility approach

Identifiers

PMID31537132
PMCPMC6758606

What OpenQuestion holds

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Registered trials

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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.