dc.creator | Elías Rodríguez, María del Pilar | es |
dc.creator | Pingitore, Valeria | es |
dc.creator | Carmona Asenjo, Ana Teresa | es |
dc.creator | Moreno Vargas, Antonio José | es |
dc.creator | Ide, Daisuke | es |
dc.creator | Miyawaki, Shota | es |
dc.creator | Kato, Atsushi | es |
dc.creator | Álvarez González, Eleuterio | es |
dc.creator | Robina Ramírez, Inmaculada | es |
dc.date.accessioned | 2019-01-25T08:15:45Z | |
dc.date.available | 2019-01-25T08:15:45Z | |
dc.date.issued | 2018 | |
dc.identifier.citation | Elías Rodríguez, M.d.P., Pingitore, V., Carmona Asenjo, A.T., Moreno Vargas, A.J., Ide, D., Miyawaki, S.,...,Robina Ramírez, I. (2018). Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry. The Journal of Organic Chemistry, 83, 8863-8873. | |
dc.identifier.issn | 1520-6904 | es |
dc.identifier.uri | https://hdl.handle.net/11441/82051 | |
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 co
ff
ee bean
α
-galactosidase
inhibitor (IC
50
= 0.37
μ
M,
K
i
= 0.12
μ
M) that has also showed
inhibition against human lysosomal
α
-galactosidase (
α
-Gal A, IC
50
=
5.3
μ
M,
K
i
= 4.2
μ
M). | es |
dc.description.sponsorship | Ministerio de Economía y Competitividad (CTQ2016-77270-R) | es |
dc.description.sponsorship | Junta de Andalucía (FQM-345) | es |
dc.format | application/pdf | es |
dc.language.iso | eng | es |
dc.publisher | American Chemical Society | es |
dc.relation.ispartof | The Journal of Organic Chemistry, 83, 8863-8873. | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
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 |
dc.type | info:eu-repo/semantics/article | es |
dcterms.identifier | https://ror.org/03yxnpp24 | |
dc.type.version | info:eu-repo/semantics/acceptedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Química orgánica | es |
dc.relation.projectID | CTQ2016-77270-R | es |
dc.relation.projectID | FQM-345 | es |
dc.relation.publisherversion | http://dx.doi.org/10.1021/acs.joc.8b01073 | es |
dc.identifier.doi | 10.1021/acs.joc.8b01073 | es |
idus.format.extent | 11 p. | es |
dc.journaltitle | The Journal of Organic Chemistry | es |
dc.publication.volumen | 83 | es |
dc.publication.initialPage | 8863 | es |
dc.publication.endPage | 8873 | es |
dc.contributor.funder | Ministerio de Economía y Competitividad (MINECO). España | |
dc.contributor.funder | Junta de Andalucía | |
dc.description.awardwinning | Premio Mensual Publicación Científica Destacada de la US. Facultad de Química | |