Evidence map›Paper›PMID 33078573›Full record

ArticleChemMedChem2021

Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases.

Daniel G Silva, Anna Junker, Shaiani M G de Melo, Fernando Fumagalli, J Robert Gillespie, Nora Molasky, Frederick S Buckner, An Matheeussen, Guy Caljon, Louis Maes and 1 more

Abstract read
In one paragraph

Article in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

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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

11 authors.

Daniel G SilvaQHeteM - Laboratório de Química Heterocíclica e Medicinal, School of Pharmaceutical Sciences of Ribeirão Preto - University of São Paulo, Ribeirão Preto, São Paulo, 14040-903, Brazil.ORCID 0000-0001-8879-456X
Anna JunkerEuropean Institute for Molecular Imaging (EIMI), Westphalian Wilhelms-University, 48149, Münster, Germany.ORCID 0000-0001-5151-0930
Shaiani M G de MeloQHeteM - Laboratório de Química Heterocíclica e Medicinal, School of Pharmaceutical Sciences of Ribeirão Preto - University of São Paulo, Ribeirão Preto, São Paulo, 14040-903, Brazil.
Fernando FumagalliCentro de Ciências da Saúde (CCS), Universidade Federal de Santa Maria (UFSM), Av. Roraima, 1000, Camobi, Santa Maria, Rio Grande do Sul, 97105-900, Brazil.ORCID 0000-0002-0622-4481
J Robert GillespieDepartment of Medicine, University of Washington, Seattle, WA, 98195, USA.ORCID 0000-0002-5650-0333
Nora MolaskyDepartment of Medicine, University of Washington, Seattle, WA, 98195, USA.
Frederick S BucknerDepartment of Medicine, University of Washington, Seattle, WA, 98195, USA.
An MatheeussenLaboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Antwerpen, 2610, Wilrijk, Belgium.
Guy CaljonLaboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Antwerpen, 2610, Wilrijk, Belgium.ORCID 0000-0002-4870-3202
Louis MaesLaboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Antwerpen, 2610, Wilrijk, Belgium.ORCID 0000-0002-2324-9509
Flavio S EmeryQHeteM - Laboratório de Química Heterocíclica e Medicinal, School of Pharmaceutical Sciences of Ribeirão Preto - University of São Paulo, Ribeirão Preto, São Paulo, 14040-903, Brazil.ORCID 0000-0002-8652-7123

Funding

Drug Discovery for Chagas DiseaseR01AI147504 · NIAID · UNIVERSITY OF WASHINGTON · PI Frederick Simmons Buckner, Michael H Gelb · 2019 to 2026
$5.9M
Conselho Nacional de Desenvolvimento Científico e Tecnológico #2017/21146-4Conselho Nacional de Desenvolvimento Científico e Tecnológico #2017/22001-0Conselho Nacional de Desenvolvimento Científico e Tecnológico #313834/2018-0Conselho Nacional de Desenvolvimento Científico e Tecnológico #428527/2016-7Conselho Nacional de Desenvolvimento Científico e Tecnológico #88881.170193/2018-01Fundacão de Amparo à Pesquisa do Estado de São Paulo (FAPESP), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil 001NIAID NIH HHS R01 AI147504
6 · The paper itself

Abstract

Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these diseases are limited, which invariably leads to fatal cases. Hence, there is an urgent need for new antitrypanosomal drugs. To address this issue, a large number of diverse heterocyclic compounds were prepared. Straightforward synthetic approaches tolerated pre-functionalized structures, giving rise to a structurally diverse set of analogs. We report on a set of 57 heterocyclic compounds with selective activity potential against kinetoplastid parasites. In general, 29 and 19 compounds of the total set could be defined as active against Trypanosoma cruzi and T. brucei brucei, respectively (antitrypanosomal activities <10 μM). The present work discusses the structure-activity relationships of new fused-ring scaffolds based on imidazopyridine/pyrimidine and furopyridine cores. This library of compounds shows significant potential for anti-trypanosomiases drug discovery.

Indexed as

Dose-Response Relationship, DrugHumansImidazolesMolecular StructureParasitic Sensitivity TestsPyridinesPyrimidinesStructure-Activity RelationshipTrypanocidal AgentsTrypanosoma brucei bruceiTrypanosoma cruziTrypanosomiasisImidazolesimidazopyridinePyridinesPyrimidinesTrypanocidal AgentsAnti-infectivesheterocyclicin vitroT. bruceiT. cruzi

Identifiers

PMID33078573
PMCPMC8048860

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.