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Título : Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis
Autor : Barreiro-Costa, Olalla
Morales-Noboa, Gabriela
Rojas-Silva, Patricio
Lara-Barba, Eliana
Santamaría-Aguirre, Javier
Bailón-Moscoso, Natalia
Romero-Benavides, Juan Carlos
Herrera, Ana
Cueva, Cristina
Ron-Garrido, Lenin
Poveda, Ana
Heredia-Moya, Jorge
Palabras clave : Bis(spiropyrazolone)cyclopropanes
Drugs
Leishmaniasis cytotoxicity
ADME
Fecha de publicación : 17-ago-2021
Citación : Barreiro-Costa, O., Morales-Noboa, G., Rojas-Silva, P., Lara-Barba, E., Santamaría-Aguirre, J., Bailón-Moscoso, N., … Heredia-Moya, J. (2021). Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis. Molecules, 26(16), 4960. doi:10.3390/molecules26164960
Resumen : This work focuses on the search and development of drugs that may become new alterna- tives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eu- karyotic models—S. cerevisiae, five cancer cell lines, and the parasite L. mexicana—were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other proper- ties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.
URI : http://www.dspace.uce.edu.ec/handle/25000/24468
ISSN : 1420-3049
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