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  4. Novel [1,2,3] triazolo[1,5-a]pyridine derivatives are trypanocidal by sterol biosynthesis pathway alteration
 
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Novel [1,2,3] triazolo[1,5-a]pyridine derivatives are trypanocidal by sterol biosynthesis pathway alteration

ISSN
1756-8919
Date Issued
2019
Author(s)
Moncada-Basualto, M 
Departamento de Ciencias del Ambiente 
Abarca, Belen
Aguilera-Venegas, Benjamin
Ballesteros, Rafael
Ballesteros-Garrido, Rafael
Gonzalez-Herrera, Fabiola
Guzman-Rivera, Daniela
Kemmerling, Ulrike
Lapier, Michel
Maya, Juan D.
Moncada-Basualto, Mauricio
Olea-Azar, Claudio
Pesce, Barbara
DOI
https://doi.org/10.4155/fmc-2018-0242
Abstract
Aim: To study a new series of [1,2,3]triazolo[1,5-α]pyridine derivatives as trypanocidal agents because current antichagasic pharmacologic therapy is only partially effective. Materials & methods: The effect of the series upon Trypanosoma cruzi epimastigotes and murine macrophages viability, cell cycle, cell death and on the metabolites of the sterol biosynthesis pathway was measured; also, docking in 14α-demethylase was analyzed. Results: Compound 16 inhibits 14α-demethylase producing an imbalance in the cholesterol/ergosterol synthesis pathway, as suggested by a metabolic control and theoretical docking analysis. Consequently, it prevented cell proliferation, stopping the cellular cycle at the G2/M phase, inducing cell death. Conclusion: Although the exact cell death mechanism remained elusive, this series can be used for the further rational design of novel antiparasitic molecules. © 2019 Newlands Press.
Subjects

14α-demethylase

cell cycle arrest

mass spectrometry

squalene/cholesterol-...

triazolopyridine deri...

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