Evidence map›Paper›PMID 30703745›Full record

ReviewEuropean journal of medicinal chemistry2019

1,2,4-Triazolo[1,5-a]pyrimidines in drug design.

Killian Oukoloff, Bobby Lucero, Karol R Francisco, Kurt R Brunden, Carlo Ballatore

Abstract readReview
In one paragraph

Review in European journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed, 1 pooled it
–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

23 citing papers in PubMed, 1 synthesis or guideline pooled it.

  1. Pooled it
  2. Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Design, synthesis, andRSC advances · 2024
    Article
  9. Article
  10. Pyrazolo - Pyrimidines as Targeted Anticancer Scaffolds - A Comprehensive Review.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2024
    Review
  11. Novel Substituted Azoloazines with Anticoagulant Activity.International journal of molecular sciences · 2023
    Article
  12. Article
  13. Article
  14. Review
  15. Article
  16. Article
  17. Article
  18. Article
  19. Article
  20. Pyrimido[1,2-Chemistry of heterocyclic compounds · 2021
    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

5 authors.

Killian OukoloffSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.
Bobby LuceroDepartment of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.
Karol R FranciscoDepartment of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.
Kurt R BrundenCenter for Neurodegenerative Disease Research, Perelman School of Medicine, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA, 19104-6323, USA.
Carlo BallatoreSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA. Electronic address: cballatore@ucsd.edu.

Funding

Orally-absorbed, small molecule microtubule-stabilizers for tauopathy treatmentR01AG044332 · NIA · UNIVERSITY OF PENNSYLVANIA · PI BALLATORE, CARLO, BRUNDEN, KURT R. · 2013 to 2017
$2.3M
Brain Penetrant Microtubule-Stabilizers to Treat CNS-invasive Parasitic DiseasesR21AI141210 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BALLATORE, CARLO, CAFFREY, CONOR · 2019 to 2020
$441k
Brain Penetrant Microtubule-Stabilizers to treat CNS-invasive parasitic diseasesR21AI133394 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BALLATORE, CARLO, CAFFREY, CONOR · 2018 to 2019
$426k
NIAID NIH HHS R21 AI133394NIAID NIH HHS R21 AI141210NIA NIH HHS R01 AG044332
6 · The paper itself

Abstract

The 1,2,4-triazolo[1,5-a]pyrimidine (TP) heterocycle, in spite of its relatively simple structure, has proved to be remarkably versatile as evidenced by its use in many different applications reported over the years in different areas of drug design. For example, as the ring system of TPs is isoelectronic with that of purines, this heterocycle has been proposed as a possible surrogate of the purine ring. However, depending on the choice of substituents, the TP ring has also been described as a potentially viable bio-isostere of the carboxylic acid functional group and of the N-acetyl fragment of ε-N-acetylated lysine. In addition, the metal-chelating properties of the TP ring have also been exploited to generate candidate treatments for cancer and parasitic diseases. In the present review article, we discuss recent applications of the TP scaffold in medicinal chemistry, and provide an overview of its properties and methods of synthesis.

Indexed as

AnimalsChemistry, PharmaceuticalDrug DesignHumansNeoplasmsParasitic DiseasesPyrimidinesStructure-Activity RelationshipTriazolesPyrimidinesTriazoles1,2,4-triazolo[1,5-a]pyrimidineHeterocyclic chemistryMedicinal chemistry

Identifiers

PMID30703745
PMCPMC6394845

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.