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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Elías-Rodríguez, Pilar | es_ES |
dc.contributor.author | Pingitore, Valeria | es_ES |
dc.contributor.author | Carmona, Ana T. | es_ES |
dc.contributor.author | Moreno-Vargas, Antonio J. | es_ES |
dc.contributor.author | Ide, Daisuke | es_ES |
dc.contributor.author | Miyawaki, Shota | es_ES |
dc.contributor.author | Kato, Atsushi | es_ES |
dc.contributor.author | Álvarez, Eleuterio | es_ES |
dc.contributor.author | Robina, Inmaculada | es_ES |
dc.date.accessioned | 2019-09-13T11:21:11Z | - |
dc.date.available | 2019-09-13T11:21:11Z | - |
dc.date.issued | 2018-08-17 | - |
dc.identifier.citation | Journal of Organic Chemistry 83(16): 8863-8873 (2018) | es_ES |
dc.identifier.issn | 0022-3263 | - |
dc.identifier.uri | http://hdl.handle.net/10261/190684 | - |
dc.description.abstract | The parallel synthesis of a 26-membered-library of aromatic/aliphatic-(thio)urea-linked pyrrolizidines followed by in situ biological evaluation toward α-galactosidases has been carried out. The combination of the (thio)urea-forming click reaction and the in situ screening is pioneer in the search for glycosidase inhibitors and has allowed the discovery of a potent coffee bean α-galactosidase inhibitor (IC50 = 0.37 μM, Ki = 0.12 μM) that has also showed inhibition against human lysosomal α-galactosidase (α-Gal A, IC50 = 5.3 μM, Ki = 4.2 μM). | es_ES |
dc.description.sponsorship | This work was supported by the Ministerio de Economía y Competitividad of Spain (CTQ2016-77270-R) and the Consejería de Economía y Conocimiento-Junta de Andalucía (FQM-345). P.E.-R. acknowledges the Spanish government for a FPU fellowship. We thank Dr. E. Moreno-Clavijo for helpful discussions and CITIUS-University of Seville (MS and NMR services) for technical assistance. This work was also supported in part by a Grant-in-Aid for Scientific Research (C) from the Japanese Society for the Promotion of Science (JSPS KAKENHI grant number JP17K08362) (A.K.). | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Chemical Society | es_ES |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/CTQ2016-77270-R | es_ES |
dc.rights | closedAccess | es_ES |
dc.title | Discovery of a potent α-Galactosidase inhibitor by in situ analysis of a library of pyrrolizidine–(Thio)urea hybrid molecules generated via click chemistry | es_ES |
dc.type | artículo | es_ES |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | https://doi.org/10.1021/acs.joc.8b01073 | es_ES |
dc.identifier.e-issn | 1520-6904 | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | es_ES |
dc.contributor.funder | Junta de Andalucía | es_ES |
dc.contributor.funder | Universidad de Sevilla | es_ES |
dc.contributor.funder | Japan Society for the Promotion of Science | es_ES |
dc.relation.csic | Sí | es_ES |
oprm.item.hasRevision | no ko 0 false | * |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100001691 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/100009042 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100011011 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.languageiso639-1 | en | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | none | - |
item.fulltext | No Fulltext | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
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