@misc{10481/63923,
year = {2020},
url = {http://hdl.handle.net/10481/63923},
abstract = {In summary, we identified that compounds 4 and 7 showed better
trypanocidal properties in vitro than BZN, with higher activity, a larger
spectrum of action and lower toxicity. With respect to in vivo activity,
the treatment with compound 7 obtained promising results to fight CD,
both in the acute and chronic phases, as indicated by the different assays,
such as PCR or IS. Studies conducted in parallel to try to determine
the mechanism of action suggest that compound 4 can carry out its
effect by inhibiting the enzymes PK or PPDK of the glycosome. As for
compound 7, we suggest that its trypanocidal effect is due to the significant
depolarisation of the mitochondrial membrane, which causes
an energetic deficit and induces T. cruzi cell death by necrosis in a
mitochondrion-dependent manner, without forgetting its possible effect
as an inhibitor of lipid biosynthesis of the parasite. It is worth considering
higher doses and combined therapies (due to their different
mechanisms of action) to obtain better efficacy, even improving the
pharmacokinetics of both compounds. Therefore, we present candidate
molecules for the development of an easy-to-synthesise anti-Chagas
agent to be implemented in a further step within the preclinical phase.},
organization = {Tesis Univ. Granada.},
organization = {panish Ministry of Economy and Competitiveness (MINECO) [grant number CTQ2014-57393-C2-1P and CSD2010-00065, FEDER funds]},
organization = {Spanish Ministry of Economy, Innovation and Science [grant number P11-CTS-7651]},
organization = {Junta de Andalucia [grant number P11-CTS-07187]},
organization = {Spanish Ministry of Education [R.M-E., grant number FPU14/01537]},
organization = {Junta de Andalucia [E.M-C., postdoctoral fellowship]},
organization = {Govern de les Illes Balears [C. L., predoctoral fellowship, FSE funds]},
publisher = {Universidad de Granada},
keywords = {Química supramolecular},
keywords = {Modelo murino},
keywords = {Actividad tripanocida},
keywords = {Experimentación},
title = {Aplicación de la química supramolecular para el diseño y experimentación en modelo murino de compuestos con actividad tripanocida},
author = {Martín-Escolano, Rubén},
}