TY - JOUR
T1 - Synthesis and evaluation of biological activities of bis(Spiropyrazolone)cyclopropanes
T2 - A potential application against Leishmaniasis
AU - Barreiro-Costa, Olalla
AU - Morales-Noboa, Gabriela
AU - Rojas-Silva, Patricio
AU - Lara-Barba, Eliana
AU - Santamaría-Aguirre, Javier
AU - Bailón-Moscoso, Natalia
AU - Romero-Benavides, Juan Carlos
AU - Herrera, Ana
AU - Cueva, Cristina
AU - Ron-Garrido, Lenin
AU - Poveda, Ana
AU - Heredia-Moya, Jorge
N1 - Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2021/8/2
Y1 - 2021/8/2
N2 - 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.
AB - 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.
KW - ADME
KW - Bis(spiropyrazolone)cyclopropanes
KW - Drugs
KW - Leishmaniasis cytotoxicity
UR - http://www.scopus.com/inward/record.url?scp=85113503969&partnerID=8YFLogxK
U2 - 10.3390/molecules26164960
DO - 10.3390/molecules26164960
M3 - Article
C2 - 34443548
AN - SCOPUS:85113503969
SN - 1420-3049
VL - 26
JO - Molecules
JF - Molecules
IS - 16
M1 - 4960
ER -
