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Title: In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
Authors: Moreno-Viguri, Elsa
Jiménez-Montes, Carmen
Martín-Escolano, Rubén
Santivañez-Veliz, Mery
Martin-Montes, Alvaro
Azqueta, Amaya
Jimenez-Lopez, Marina
Zamora Ledesma, Salvador
Cirauqui, Nuria
López de Ceráin, Adela
Marín, Clotilde
Sánchez-Moreno, Manuel
Pérez-Silanes, Silvia
metadata.dc.subject.mesh: Animals
Cells, Cultured
Chagas Disease
Chlorocebus aethiops
Disease Models, Animal
Dose-Response Relationship, Drug
Mannich Bases
Mice, Inbred BALB C
Molecular Structure
Parasitic Sensitivity Tests
Structure-Activity Relationship
Trypanocidal Agents
Trypanosoma cruzi
Vero Cells
Issue Date: 6-Dec-2016
Abstract: Chagas disease is a neglected tropical disease with 6-7 million people infected worldwide, and there is no effective treatment. Therefore, there is an urgent need to continue researching in order to discover novel therapeutic alternatives. We present a series of arylaminoketone derivatives as means of identifying new drugs to treat Chagas disease in the acute phase with greater activity, less toxicity, and a larger spectrum of action than that corresponding to the reference drug benznidazole. Indexes of high selectivity found in vitro formed the basis for later in vivo assays in BALB/c mice. Murine model results show that compounds 3, 4, 7, and 10 induced a remarkable decrease in parasitemia levels in acute phase and the parasitemia reactivation following immunosuppression, and curative rates were higher than with benznidazole. These high antiparasitic activities encourage us to propose these compounds as promising molecules for developing an easy to synthesize anti-Chagas agent.
metadata.dc.identifier.doi: 10.1021/acs.jmedchem.6b00784
Appears in Collections:Producción 2020

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