Evidence map›Paper›PMID 40666484›Full record

ArticleACS medicinal chemistry letters2025

Scaffold Hopping Strategy toward New 4‑Aminoquinazolines Active Against Extracellular and Intracellular.

Guilherme Arraché Gonçalves, Alexia de Matos Czeczot, Marcia Alberton Perelló, Eric Greve, Renee Allen, Camili Zanella Zotti, Laura Calle González, Andresa Berger, Josiane Delgado Paz, Lídia Klatt Oliveira and 5 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

15 authors.

Guilherme Arraché GonçalvesInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Alexia de Matos CzeczotInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Marcia Alberton PerellóInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Eric GreveCenter for Global Infectious Disease Research, Seattle Children's Research Institute, Seattle, Washington 98101, United States of America.
Renee AllenCenter for Global Infectious Disease Research, Seattle Children's Research Institute, Seattle, Washington 98101, United States of America.
Camili Zanella ZottiInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Laura Calle GonzálezInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Andresa BergerInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Josiane Delgado PazInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Lídia Klatt OliveiraInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.
Sidnei Moura E SilvaLaboratório de Biotecnologia de Produtos Naturais e Sintéticos, Universidade de Caxias do Sul, 95070-560 Caxias do Sul, Rio Grande do Sul, Brazil.ORCID https://orcid.org/0000-0003-1903-6735
Cristiano Valim BizarroInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.ORCID https://orcid.org/0000-0002-2609-8996
Luiz Augusto BassoInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.ORCID https://orcid.org/0000-0003-0903-2407
Tanya ParishCenter for Global Infectious Disease Research, Seattle Children's Research Institute, Seattle, Washington 98101, United States of America.ORCID https://orcid.org/0000-0001-7507-0423
Pablo MachadoInstituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, 90616-900 Porto Alegre, Rio Grande do Sul, Brazil.ORCID https://orcid.org/0000-0001-5616-9583

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A series of 4-aminoquinazolines was designed through a scaffold hopping approach inspired by pharmacophoric features of known antimycobacterial agents. The compounds were synthesized via a one-pot silylation-amination reaction under solvent-free conditions, affording the desired molecules in 70%-99% yields. Antimycobacterial evaluation using multiple strains and assay platforms revealed potent activity, with MIC values as low as 0.28 μM. Structure-activity relationship analysis identified the

Indexed as

Drug designIntracellular activityMycobacterium tuberculosisQuinazolinesStructure−activity relationship

Identifiers

PMID40666484
PMCPMC12257397

What OpenQuestion holds

Textmetadata
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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.