Evidence map›Paper›PMID 25580906›Full record

ArticleJournal of medicinal chemistry2015

Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.

Maria V Papadopoulou, William D Bloomer, Galina I Lepesheva, Howard S Rosenzweig, Marcel Kaiser, Benjamín Aguilera-Venegas, Shane R Wilkinson, Eric Chatelain, Jean-Robert Ioset

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing 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

17 citing papers in PubMed.

  1. Review
  2. Review
  3. Anti-Molecules (Basel, Switzerland) · 2023
    Article
  4. Article
  5. Article
  6. An insight on medicinal attributes of 1,2,4-triazoles.European journal of medicinal chemistry · 2020
    Review
  7. Fluconazole analogues with metal-binding motifs impact metal-dependent processes and demonstrate antifungal activity in Candida albicans.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020
    Article
  8. Article
  9. Current trends in the pharmacological management of Chagas disease.International journal for parasitology. Drugs and drug resistance · 2020
    Review
  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.European journal of medicinal chemistry · 2016
    Article
  17. 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.

Maria V PapadopoulouNorthShore University HealthSystem , Evanston, Illinois 60201, United States.
William D Bloomer
Galina I Lepesheva
Howard S Rosenzweig
Marcel Kaiser
Benjamín Aguilera-Venegas
Shane R Wilkinson
Eric Chatelain
Jean-Robert Ioset

Funding

Structural Requirements for Sterol 14alpha-DemethylasesR01GM067871 · NIGMS · VANDERBILT UNIVERSITY · PI LEPESHEVA, GALINA I · 2004 to 2023
$7.2M
NIGMS NIH HHS GM067871NIGMS NIH HHS R01 GM067871
6 · The paper itself

Abstract

3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductase (NTR) located in the mitochondrion of trypanosomatids and, at the same time, act as inhibitors of the sterol 14α-demethylase (T. cruzi CYP51) enzyme. Because combination treatments against parasites are often superior to monotherapy, we believe that this emerging class of bifunctional compounds may introduce a new generation of antitrypanosomal drugs. In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed.

Indexed as

AmidesAnimalsCell LineChagas DiseaseDose-Response Relationship, DrugMethanolMiceMice, Inbred BALB CMolecular StructureParasitic Sensitivity TestsRatsStructure-Activity RelationshipTriazolesTrypanocidal AgentsTrypanosoma brucei rhodesienseTrypanosoma cruziAmidesMethanolTriazolesTrypanocidal Agents

Identifiers

PMID25580906
PMCPMC4337820

What OpenQuestion holds

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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.