{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,10]],"date-time":"2026-09-10T07:14:36Z","timestamp":1789024476527,"version":"build-2803163510"},"reference-count":66,"publisher":"MDPI AG","issue":"16","license":[{"start":{"date-parts":[[2021,8,17]],"date-time":"2021-08-17T00:00:00Z","timestamp":1629158400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Corporaci\u00f3n Ecuatoriana para el Desarrollo de la Investigaci\u00f3n y la Academia (CEDIA)","award":["CEPRA XI-2017-10"],"award-info":[{"award-number":["CEPRA XI-2017-10"]}]},{"name":"Universidad UTE","award":["SN"],"award-info":[{"award-number":["SN"]}]},{"name":"Universidad Central del Ecuador","award":["Direcci\u00f3n General de Investigaci\u00f3n y Proyectos-DGIP, project #6"],"award-info":[{"award-number":["Direcci\u00f3n General de Investigaci\u00f3n y Proyectos-DGIP, project #6"]}]},{"name":"SENPLADES","award":["9175.0000.0000.377784 and 91750000.0000.375239"],"award-info":[{"award-number":["9175.0000.0000.377784 and 91750000.0000.375239"]}]},{"name":"Acad\u00e9mie de Recherche et d\u00b4Enseignement Sup\u00e9rieur (ARES)","award":["SN"],"award-info":[{"award-number":["SN"]}]},{"name":"Universidad T\u00e9cnica Particular de Loja","award":["PROY_INV_QUI_2017_2222"],"award-info":[{"award-number":["PROY_INV_QUI_2017_2222"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>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\u2014S. cerevisiae, five cancer cell lines, and the parasite L. mexicana\u2014were 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.<\/jats:p>","DOI":"10.3390\/molecules26164960","type":"journal-article","created":{"date-parts":[[2021,8,17]],"date-time":"2021-08-17T03:43:04Z","timestamp":1629171784000},"page":"4960","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis"],"prefix":"10.3390","volume":"26","author":[{"given":"Olalla","family":"Barreiro-Costa","sequence":"first","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica (CENBIO), Facultad de Ciencias de la Salud Eugenio Espejo, Universidad UTE, Quito 170527, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gabriela","family":"Morales-Noboa","sequence":"additional","affiliation":[{"name":"DNA Replication and Genome Instability Unit, Grupo de Investigaci\u00f3n en Biodiversidad, Zoonosis y Salud P\u00fablica (GIBCIZ), Instituto de Investigaci\u00f3n en Zoonosis-CIZ, Facultad de Ciencias Qu\u00edmicas, Facultad de Ciencias Agr\u00edcolas, Universidad Central del Ecuador, Quito 170521, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Patricio","family":"Rojas-Silva","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica (CENBIO), Facultad de Ciencias de la Salud Eugenio Espejo, Universidad UTE, Quito 170527, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5148-9959","authenticated-orcid":false,"given":"Eliana","family":"Lara-Barba","sequence":"additional","affiliation":[{"name":"DNA Replication and Genome Instability Unit, Grupo de Investigaci\u00f3n en Biodiversidad, Zoonosis y Salud P\u00fablica (GIBCIZ), Instituto de Investigaci\u00f3n en Zoonosis-CIZ, Facultad de Ciencias Qu\u00edmicas, Facultad de Ciencias Agr\u00edcolas, Universidad Central del Ecuador, Quito 170521, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1683-5737","authenticated-orcid":false,"given":"Javier","family":"Santamar\u00eda-Aguirre","sequence":"additional","affiliation":[{"name":"DNA Replication and Genome Instability Unit, Grupo de Investigaci\u00f3n en Biodiversidad, Zoonosis y Salud P\u00fablica (GIBCIZ), Instituto de Investigaci\u00f3n en Zoonosis-CIZ, Facultad de Ciencias Qu\u00edmicas, Facultad de Ciencias Agr\u00edcolas, Universidad Central del Ecuador, Quito 170521, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2754-1328","authenticated-orcid":false,"given":"Natalia","family":"Bail\u00f3n-Moscoso","sequence":"additional","affiliation":[{"name":"Departamento de Ciencias de la Salud, Universidad T\u00e9cnica Particular de Loja, Loja 1101608, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1660-1217","authenticated-orcid":false,"given":"Juan Carlos","family":"Romero-Benavides","sequence":"additional","affiliation":[{"name":"Departamento de Qu\u00edmica, Universidad T\u00e9cnica Particular de Loja, Loja 1101608, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ana","family":"Herrera","sequence":"additional","affiliation":[{"name":"Departamento de Ciencias de la Salud, Universidad T\u00e9cnica Particular de Loja, Loja 1101608, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cristina","family":"Cueva","sequence":"additional","affiliation":[{"name":"Departamento de Ciencias de la Salud, Universidad T\u00e9cnica Particular de Loja, Loja 1101608, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lenin","family":"Ron-Garrido","sequence":"additional","affiliation":[{"name":"DNA Replication and Genome Instability Unit, Grupo de Investigaci\u00f3n en Biodiversidad, Zoonosis y Salud P\u00fablica (GIBCIZ), Instituto de Investigaci\u00f3n en Zoonosis-CIZ, Facultad de Ciencias Qu\u00edmicas, Facultad de Ciencias Agr\u00edcolas, Universidad Central del Ecuador, Quito 170521, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1505-1372","authenticated-orcid":false,"given":"Ana","family":"Poveda","sequence":"additional","affiliation":[{"name":"DNA Replication and Genome Instability Unit, Grupo de Investigaci\u00f3n en Biodiversidad, Zoonosis y Salud P\u00fablica (GIBCIZ), Instituto de Investigaci\u00f3n en Zoonosis-CIZ, Facultad de Ciencias Qu\u00edmicas, Facultad de Ciencias Agr\u00edcolas, Universidad Central del Ecuador, Quito 170521, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7620-9140","authenticated-orcid":false,"given":"Jorge","family":"Heredia-Moya","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica (CENBIO), Facultad de Ciencias de la Salud Eugenio Espejo, Universidad UTE, Quito 170527, Ecuador"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,8,17]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"7","DOI":"10.1007\/s10593-012-0960-z","article-title":"Heterocycles in drugs and drug discovery","volume":"48","author":"Gomtsyan","year":"2012","journal-title":"Chem. 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