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Journal Articles European Journal of Medicinal Chemistry Year : 2016

New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease

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Abstract

Herein, we describe a new approach towards the synthesis of selenosemicarbazones. The reaction involves an O-Se exchange of semicarbazones using Ishihara reagent. Eleven selenosemicarbazones were prepared using this methodology, with low to moderate yields. Among the prepared compounds the m-bromo phenyl methyl derivative 1b was selected to be evaluated in vivo, in a murine model of acute Chagas' disease. Compound 1b 10 mg/kg bw/day reduced 50% of parasitaemia profile compared with the control group, but was less effective than Benznidazole (50 mg/kg bw/day reduced 90%) and toxic. These studies are important to guide future Chagas drug design.
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pasteur-01882348 , version 1 (26-09-2018)

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Chiara Pizzo, Paula Faral-Tello, Gloria Yaluff, Elva Serna, Susana Torres, et al.. New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease. European Journal of Medicinal Chemistry, 2016, 109, pp.107 - 113. ⟨10.1016/j.ejmech.2015.12.040⟩. ⟨pasteur-01882348⟩
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