Jimenez-Lopez, M. (Marina)

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    In vitro and in vivo anti-Trypanosoma cruzi activity of new arylamine Mannich base-type derivatives
    (2016) Jimenez-Montes, C. (Carmen); Martin-Escolano, R. (Ruben); Lopez-de-Cerain, A. (Adela); Pérez-Silanes, S. (Silvia); Zamora-Ledesma, S. (Salvador); Sanchez-Moreno, M. (Manuel); Marin, C. (Clotilde); Cirauqui, N. (Nuria); Moreno-de-Viguri, E. (Elsa); Jimenez-Lopez, M. (Marina); Santivañez-Veliz, M. (Mery); Martin-Montes, A.(Alvaro); Azqueta, A. (Amaya)
    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 with 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 anti-parasitic activities encourage us to propose these compounds as promising molecules for developing an easy to synthesize anti-Chagas agent.