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Biomed Pharmacother ; 108: 1703-1711, 2018 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30372873

RESUMEN

Chagas disease is a major health problem not only in Latin America but also in Europe and North America due to the spread of this disease into nonendemic areas. In terms of global burden, this major tropical infection is considered to be one of the most neglected diseases, and there are currently only two available chemotherapies: benznidazole and nifurtimox. Unfortunately, although these chemotherapies are beneficial in the acute phase of the disease, benznidazole and nifurtimox lead to significant side effects, including hepatitis and neurotoxicity. Therefore, the search for and development of more effective, safe and inexpensive anti-Trypanosoma cruzi drugs are required. In this work, a series of 10 nitroaromatic Schiff bases bearing different (nitro) aromatic rings-was synthesized. Subsequently, the in vitro and in vivo anti-T. cruzi activities of the Schiff bases were investigated, as well as the in vivo toxicity and the biological effects. The basic structure of the most promising in vivo Schiff base, 10 would be useful in the synthesis of new compounds for Chagas disease treatment.


Asunto(s)
Hidrocarburos Aromáticos/farmacología , Bases de Schiff/síntesis química , Bases de Schiff/farmacología , Pruebas de Toxicidad , Tripanocidas/síntesis química , Tripanocidas/farmacología , Trypanosoma cruzi/efectos de los fármacos , Administración Oral , Animales , Femenino , Hidrocarburos Aromáticos/síntesis química , Hidrocarburos Aromáticos/química , Hidrocarburos Aromáticos/toxicidad , Hígado/efectos de los fármacos , Hígado/patología , Ratones , Parasitemia/tratamiento farmacológico , Bases de Schiff/química , Bases de Schiff/toxicidad , Tripanocidas/química , Tripanocidas/toxicidad
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