ARTÍCULO

In vitro and in vivo anti-Trypanosoma cruzi activity of new arylamine Mannich base-type derivatives

Autores: Moreno de Viguri, Elsa; Jiménez-Montes, C.; Martín-Escolano, R.; Santivañez Veliz, Mery Jhenny; Martín-Montes, A.; Azqueta Oscoz, Amaya; Jiménez-López, M.; Zamora-Ledesma, S.; Cirauqui, N.; López de Cerain Salsamendi, Adela; Marín, C.; Sánchez-Moreno, M.; Pérez Silanes, Silvia
Título de la revista: JOURNAL OF MEDICINAL CHEMISTRY
ISSN: 0022-2623
Volumen: 59
Número: 24
Páginas: 10929 - 10945
Fecha de publicación: 2016
Resumen:
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.