Development of Novel Isoindolone-Based Compounds against Trypanosoma brucei rhodesiense.


Journal

ChemistryOpen
ISSN: 2191-1363
Titre abrégé: ChemistryOpen
Pays: Germany
ID NLM: 101594811

Informations de publication

Date de publication:
09 2021
Historique:
revised: 02 09 2021
received: 21 07 2021
entrez: 23 9 2021
pubmed: 24 9 2021
medline: 4 1 2022
Statut: ppublish

Résumé

This study identified the isoindolone ring as a scaffold for novel agents against Trypanosoma brucei rhodesiense and explored the structure-activity relationships of various aromatic ring substitutions. The compounds were evaluated in an integrated in vitro screen. Eight compounds exhibited selective activity against T. b. rhodesiense (IC

Identifiants

pubmed: 34553828
doi: 10.1002/open.202100180
pmc: PMC8459400
doi:

Substances chimiques

Isoindoles 0
Trypanocidal Agents 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

922-927

Subventions

Organisme : Fundacão de Amparo à Pesquisa do Estado de São Paulo
Organisme : Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil
ID : 001
Organisme : Conselho Nacional de Desenvolvimento Científico e Tecnológico
ID : 88881.170193/2018-01
Organisme : Conselho Nacional de Desenvolvimento Científico e Tecnológico
ID : 2017/22001-0
Organisme : Conselho Nacional de Desenvolvimento Científico e Tecnológico
ID : 2017/21146-4
Organisme : Conselho Nacional de Desenvolvimento Científico e Tecnológico
ID : 313834/2018-0
Organisme : Conselho Nacional de Desenvolvimento Científico e Tecnológico
ID : 428527/2016-7

Informations de copyright

© 2021 The Authors. Published by Wiley-VCH GmbH.

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Auteurs

Daniel G Silva (DG)

QHeteM - Laboratório de Química Heterocíclica e Medicinal, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, 14040-903, Brazil.
European Institute for Molecular Imaging (EIMI), Westphalian Wilhelms-University Münster, 48149, Münster, Germany.

Pim-Bart Feijens (PB)

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Wilrijk B, 2610, Belgium.

Rik Hendrickx (R)

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Wilrijk B, 2610, Belgium.

An Matheeussen (A)

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Wilrijk B, 2610, Belgium.

Lucie Grey (L)

Institute for Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms-University Münster, 48149, Münster, Germany.

Guy Caljon (G)

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Wilrijk B, 2610, Belgium.

Louis Maes (L)

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, Wilrijk B, 2610, Belgium.

Flavio S Emery (FS)

QHeteM - Laboratório de Química Heterocíclica e Medicinal, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, 14040-903, Brazil.

Anna Junker (A)

European Institute for Molecular Imaging (EIMI), Westphalian Wilhelms-University Münster, 48149, Münster, Germany.

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Classifications MeSH