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ChemMedChem ; 16(23): 3600-3614, 2021 12 06.
Artículo en Inglés | MEDLINE | ID: mdl-34665510

RESUMEN

Leishmaniasis and Chagas diseases are two of the most important parasitic diseases in the world. Both belong to the category of Neglected Tropical Diseases, and they cannot be prevented by vaccination. Their treatments are founded in outdated drugs that possess many pernicious side-effects and they're not easy to administer. With the aim of discovering new compounds that could serve as anti-trypanosomal drugs, an antiparasitic study of a synthetic compound family has been conducted. A series of new 1,4-bis(alkylamino)- and 1-alkylamino-4-chloroazine and benzoazine derivatives 1-4 containing imidazole rings have been synthesized and identified. Their structures showed a possible interest based on previous work. Their in vitro anti-Leishmania infantum, anti-L. braziliensis, anti-L. donovani and anti-T. cruzi activity were tested, as well as the inhibition of Fe-SOD enzymes. It was found that some of them exhibited quite relevant values indicative of being worthy of future more detailed studies, as most of them showed activity to more than only one parasite species, especially compound 3 c was active for the three studied Leishmania species and also for T. cruzi, which is a very interesting trait as it covers a wide spectrum.


Asunto(s)
Imidazoles/farmacología , Ftalazinas/farmacología , Piridazinas/farmacología , Tripanocidas/farmacología , Animales , Chlorocebus aethiops , Imidazoles/síntesis química , Imidazoles/toxicidad , Leishmania braziliensis/efectos de los fármacos , Leishmania donovani/efectos de los fármacos , Leishmania infantum/efectos de los fármacos , Pruebas de Sensibilidad Parasitaria , Ftalazinas/síntesis química , Ftalazinas/toxicidad , Piridazinas/síntesis química , Piridazinas/toxicidad , Tripanocidas/síntesis química , Tripanocidas/toxicidad , Trypanosoma cruzi/efectos de los fármacos , Células Vero
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