Evidence map›Paper›PMID 28629306›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2017

β-CA-specific inhibitor dithiocarbamate Fc14-584B: a novel antimycobacterial agent with potential to treat drug-resistant tuberculosis.

Ashok Aspatwar, Milka Hammarén, Sanni Koskinen, Bruno Luukinen, Harlan Barker, Fabrizio Carta, Claudiu T Supuran, Mataleena Parikka, Seppo Parkkila

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.

0numbers the graph read from it
0cells of the map it votes in
36citing papers in PubMed
2.0field-weighted citation impact, top 13% 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

36 citing papers in PubMed, 56 citations in OpenAlex.

  1. Review
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  12. Novel Drug Screening Assay forJournal of medicinal chemistry · 2024
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  13. Article
  14. Selected strategies to fight pathogenic bacteria.Journal of enzyme inhibition and medicinal chemistry · 2023
    Review
  15. Article
  16. Medicinal Plants as Therapeutic Alternatives to CombatAntibiotics (Basel, Switzerland) · 2023
    Review
  17. Review
  18. Article
  19. Article
  20. 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

9 authors at 3 institutions in 2 countries.

Ashok Aspatwara Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Milka Hammaréna Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Sanni Koskinena Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Bruno Luukinena Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Harlan Barkera Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Fabrizio Cartab Neurofarba Department , Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.
Claudiu T Supuranb Neurofarba Department , Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.
Mataleena Parikkaa Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Seppo Parkkilaa Faculty of Medicine and Life Sciences , University of Tampere , Tampere , Finland.
Tampere University · FIUniversity of Florence · ITTampere University · FI

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibition of novel biological pathways in Mycobacterium tuberculosis (Mtb) creates the potential for alternative approaches for treating drug-resistant tuberculosis. In vitro studies have shown that dithiocarbamate-derived β-carbonic anhydrase (β-CA) inhibitors Fc14-594 A and Fc14-584B effectively inhibit the activity of Mtb β-CA enzymes. We screened the dithiocarbamates for toxicity, and studied the in vivo inhibitory effect of the least toxic inhibitor on M. marinum in a zebrafish model. In our toxicity screening, Fc14-584B emerged as the least toxic and showed minimal toxicity in 5-day-old larvae at 300 µM concentration. In vitro inhibition of M. marinum showed that both compounds inhibited growth at a concentration of 75 µM. In vivo inhibition studies using 300 µM Fc14-584B showed significant (p > .05) impairment of bacterial growth in zebrafish larvae at 6 days post infection. Our studies highlight the therapeutic potential of Fc14-584B as a β-CA inhibitor against Mtb, and that dithiocarbamate compounds may be developed into potent anti-tuberculosis drugs.

Indexed as

AnimalsAntitubercular AgentsCarbonic Anhydrase InhibitorsCarbonic AnhydrasesDose-Response Relationship, DrugLarvaMicrobial Sensitivity TestsMycobacterium tuberculosisPiperazinesStructure-Activity RelationshipThiocarbamatesTuberculosis, Multidrug-ResistantZebrafishAntitubercular AgentsCarbonic Anhydrase InhibitorsCarbonic AnhydrasesFc14-584BPiperazinesThiocarbamatesDithiocarbamatesin vivo inhibitionMycobacterium marinumzebrafish embryosβ-carbonic anhydrase

Identifiers

PMID28629306
PMCPMC6445161
OpenAlexW2710434615

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.