In vitro and in vivo anti-Trypanosoma cruzi activity of new arylamine Mannich base-type derivatives
Keywords: 
Materias Investigacion::Química
Issue Date: 
2016
Citation: 
Moreno-Viguri, E. (Elsa); Jimenez-Montes, C. (Carmen); Martin-Escolano, R. (Ruben); et al. "In vitro and in vivo anti-Trypanosoma cruzi activity of new arylamine Mannich base-type derivatives". J. Med. Chem. 24 (59), 2016, 10929 - 10945
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 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.

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