Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Olalla Barreiro-Costa; Gabriela Morales-Noboa; Patricio Rojas-Silva; Eliana Lara-Barba; Javier Santamaría-Aguirre; Natalia Bailón-Moscoso; Juan Carlos Romero-Benavides; Ana Herrera; Cristina Cueva; Lenin Ron-Garrido; Ana Poveda; HEREDIA MOYA, JORGE HUMBERTO

doi:10.3390/molecules26164960

Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Journal

Molecules

ISSN

1420-3049

Date Issued

2021-08-17

Author(s)

Olalla Barreiro-Costa

Facultad de Ciencias de la Salud Eugenio Espejo

Gabriela Morales-Noboa

Patricio Rojas-Silva

Facultad de Ciencias de la Salud Eugenio Espejo

Eliana Lara-Barba

Javier Santamaría-Aguirre

Natalia Bailón-Moscoso

Juan Carlos Romero-Benavides

Ana Herrera

Cristina Cueva

Lenin Ron-Garrido

Ana Poveda

HEREDIA MOYA, JORGE HUMBERTO

Facultad de Ciencias de la Salud Eugenio Espejo

DOI

10.3390/molecules26164960

URL

https://cris.ute.edu.ec/handle/123456789/527

Abstract

This work focuses on the search and development of drugs that may become new alternatives 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 eukaryotic 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 properties 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.