Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis.
ChemMedChem
; 13(17): 1751-1754, 2018 09 06.
Article
em En
| MEDLINE
| ID: mdl-29969537
ABSTRACT
In vitro whole-organism screens of Trypanosoma brucei with representative examples of brain-penetrant microtubule (MT)-stabilizing agents identified lethal triazolopyrimidines and phenylpyrimidines with sub-micromolar potency. In mammalian cells, these antiproliferative compounds disrupt MT integrity and decrease total tubulin levels. Their parasiticidal potency, combined with their generally favorable pharmacokinetic properties, which include oral bioavailability and brain penetration, suggest that these compounds are potential leads against human African trypanosomiasis.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
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Tripanossomicidas
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Trypanosoma brucei brucei
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Tripanossomíase Africana
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Encéfalo
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Microtúbulos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article