Evidence map›Paper›PMID 25773920›Full record

ArticleScientific reports2015

Amide-controlled, one-pot synthesis of tri-substituted purines generates structural diversity and analogues with trypanocidal activity.

Maria J Pineda de las Infantas y Villatoro, Juan D Unciti-Broceta, Rafael Contreras-Montoya, Jose A Garcia-Salcedo, Miguel A Gallo Mezo, Asier Unciti-Broceta, Juan J Diaz-Mochon

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.5field-weighted citation impact, top 33% 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

3 citing papers in PubMed, 18 citations in OpenAlex.

  1. Identification of compounds with activity againstFrontiers in cellular and infection microbiology · 2022
    Article
  2. Novel Purine Chemotypes with Activity againstPharmaceuticals (Basel, Switzerland) · 2021
    Article
  3. 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

7 authors at 3 institutions in 2 countries.

Maria J Pineda de las Infantas y VillatoroDepartamento de Química Farmacéutica y Orgánica. University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
Juan D Unciti-BrocetaPfizer - Universidad de Granada - Junta de Andalucía Centre for Genomics and Oncological Research (GENYO), Parque Tecnológico de Ciencias de la Salud (PTS), Avenida de la Ilustración 114, 18016 Granada, Spain.
Rafael Contreras-MontoyaPfizer - Universidad de Granada - Junta de Andalucía Centre for Genomics and Oncological Research (GENYO), Parque Tecnológico de Ciencias de la Salud (PTS), Avenida de la Ilustración 114, 18016 Granada, Spain.
Jose A Garcia-Salcedo1] Pfizer - Universidad de Granada - Junta de Andalucía Centre for Genomics and Oncological Research (GENYO), Parque Tecnológico de Ciencias de la Salud (PTS), Avenida de la Ilustración 114, 18016 Granada, Spain [2] Unidad de Enfermedades Infecciosas y Microbiología, Complejo Hospitalario de Granada, Instituto de Investigación Biosanitaria de Granada, Dr. Azpitarte, 4, 18012 Granada, Spain.
Miguel A Gallo MezoDepartamento de Química Farmacéutica y Orgánica. University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain.
Asier Unciti-BrocetaEdinburgh Cancer Research UK Centre, MRC Institute of Genetics and Molecular Medicine, University of Edinburgh, Crewe Road South, Edinburgh EH4 2XR, UK.
Juan J Diaz-Mochon1] Departamento de Química Farmacéutica y Orgánica. University of Granada, Campus de Cartuja s/n, 18071 Granada, Spain [2] Pfizer - Universidad de Granada - Junta de Andalucía Centre for Genomics and Oncological Research (GENYO), Parque Tecnológico de Ciencias de la Salud (PTS), Avenida de la Ilustración 114, 18016 Granada, Spain.
Pfizer-University of Granada-Junta de Andalucía Centre for Genomics and Oncological Research · ESUniversidad de Granada · ESMRC Institute of Genetics and Molecular Medicine · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A novel one-pot synthesis of tri-substituted purines and the discovery of purine analogues with trypanocidal activity are reported. The reaction is initiated by a metal-free oxidative coupling of primary alkoxides and diaminopyrimidines with Schiff base formation and subsequent annulation in the presence of large N,N-dimethylamides (e.g. N,N-dimethylpropanamide or larger). This synthetic route is in competition with a reaction previously-reported by our group, allowing the generation of a combinatorial library of tri-substituted purines by the simple modification of the amide and the alkoxide employed. Among the variety of structures generated, two purine analogues displayed trypanocidal activity against the protozoan parasite Trypanosoma brucei with IC50 < 5 μM, being each of those compounds obtained through each of the synthetic pathways.

Indexed as

Chemistry Techniques, SyntheticAmidesPurinesTrypanocidal AgentsTrypanosoma brucei bruceiAmidespurinePurinesTrypanocidal Agents

Identifiers

PMID25773920
PMCPMC5390905
OpenAlexW2077052885

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.