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dc.contributor.authorRisi, Gastón-
dc.contributor.authorAguilera, Elena-
dc.contributor.authorLadós, Enrique-
dc.contributor.authorSuárez, Gonzalo-
dc.contributor.authorCarrera, Inés-
dc.contributor.authorÁlvarez, Guzmán-
dc.contributor.authorSalinas, Gustavo-
dc.date.accessioned2021-07-22T14:57:14Z-
dc.date.available2021-07-22T14:57:14Z-
dc.date.issued2019-
dc.identifier.citationRisi, G, Aguilera, E, Ladós, E, y otros "Caenorhabditis elegans infrared-based motility assay identified new hits for nematicide drug development". Veterinary Sciences. [en línea] 2019, 6(1): 29. 15 h. DOI: 10.3390/vetsci6010029es
dc.identifier.issn2306-7381-
dc.identifier.urihttps://hdl.handle.net/20.500.12008/28679-
dc.description.abstractNematode parasites have a profound impact on humankind, infecting nearly one-quarter of the world’s population, as well as livestock. There is a pressing need for discovering nematicides due to the spread of resistance to currently used drugs. The free-living nematode Caenorhabditis elegans is a formidable experimentally tractable model organism that offers key advantages in accelerating nematicide discovery. We report the screening of drug-like libraries using an overnight high-throughput C. elegans assay, based on an automated infrared motility reader. As a proof of concept, we screened the “Pathogen Box” library, and identical results to a previous screen using Haemonchus contortus were obtained. We then screened an in-house library containing a diversity of compound families. Most active compounds had a conjugation of an unsaturation with an electronegative atom (N, O, or S) and an aromatic ring. Importantly, we identified symmetric arylidene ketones and aryl hydrazine derivatives as novel nematicides. Furthermore, one of these compounds, (1E,2E)-1,2-bis(thiophen-3-ylmethylene)hydrazine, was active as a nematicide at 25 µm, but innocuous to the vertebrate model zebrafish at 50 µm. Our results identified novel nematicidal scaffolds and illustrate the value of C. elegans in accelerating nematicide discovery using a nonlabor-intensive automated assay that provides a simple overnight readout.en
dc.format.extent15 h.es
dc.format.mimetypeapplication/pdfes
dc.language.isoenes
dc.publisherMDPIes
dc.relation.ispartofVeterinary Sciences, 2019, 6(1): 29es
dc.rightsLas obras depositadas en el Repositorio se rigen por la Ordenanza de los Derechos de la Propiedad Intelectual de la Universidad de la República.(Res. Nº 91 de C.D.C. de 8/III/1994 – D.O. 7/IV/1994) y por la Ordenanza del Repositorio Abierto de la Universidad de la República (Res. Nº 16 de C.D.C. de 07/10/2014)es
dc.subjectNematicideen
dc.subjectNematodeen
dc.subjectAnthelminticen
dc.subjectC. elegansen
dc.subjectArylidene ketonesen
dc.subjectAryl hydrazineen
dc.subjectPathogen Boxen
dc.titleCaenorhabditis elegans infrared-based motility assay identified new hits for nematicide drug developmenten
dc.typeArtículoes
dc.contributor.filiacionRisi Gastón, Instituto Pasteur (Montevideo).-
dc.contributor.filiacionAguilera Elena, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica.-
dc.contributor.filiacionLadós Enrique, Instituto Pasteur (Montevideo).-
dc.contributor.filiacionSuárez Gonzalo, Universidad de la República (Uruguay). Facultad de Veterinaria.-
dc.contributor.filiacionCarrera Inés, Instituto Pasteur (Montevideo).-
dc.contributor.filiacionÁlvarez Guzmán, Universidad de la República (Uruguay). CENUR.-
dc.contributor.filiacionSalinas Gustavo, Instituto Pasteur (Montevideo).-
dc.rights.licenceLicencia Creative Commons Atribución (CC - By 4.0)es
dc.identifier.doi10.3390/vetsci6010029-
Aparece en las colecciones: Publicaciones académicas y científicas - Facultad de Ciencias

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