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

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 applicatio...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-08, Vol.26 (16), p.4960
Main Authors: 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
Format: Article
Language:English
Subjects:
ADME
Analgesics
Animals
Antioxidants
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
Biological activity
bis(spiropyrazolone)cyclopropanes
Cancer
Cell growth
Cell Line, Tumor
Cyclopropane
Cyclopropanes - chemical synthesis
Cyclopropanes - chemistry
Cyclopropanes - pharmacology
Cytotoxicity
Drug development
Drugs
Genotoxicity
Humans
Laboratories
Leishmania mexicana - drug effects
Leishmaniasis
Leishmaniasis - drug therapy
Leishmaniasis - parasitology
leishmaniasis cytotoxicity
Mammalian cells
Mammals
Metabolism
Molecular Structure
Organic compounds
Parasites
Saccharomyces cerevisiae - drug effects
Spiro Compounds - chemical synthesis
Spiro Compounds - chemistry
Spiro Compounds - pharmacology
Tumor cell lines
Vector-borne diseases
Yeast
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Summary: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- , five cancer cell lines, and the parasite -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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26164960