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Título: | Discovery of a potent α-Galactosidase inhibitor by in situ analysis of a library of pyrrolizidine–(Thio)urea hybrid molecules generated via click chemistry |
Autor: | Elías-Rodríguez, Pilar; Pingitore, Valeria; Carmona, Ana T.; Moreno-Vargas, Antonio J.; Ide, Daisuke; Miyawaki, Shota; Kato, Atsushi; Álvarez, Eleuterio CSIC ORCID ; Robina, Inmaculada | Fecha de publicación: | 17-ago-2018 | Editor: | American Chemical Society | Citación: | Journal of Organic Chemistry 83(16): 8863-8873 (2018) | Resumen: | 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). | Versión del editor: | https://doi.org/10.1021/acs.joc.8b01073 | URI: | http://hdl.handle.net/10261/190684 | ISSN: | 0022-3263 | E-ISSN: | 1520-6904 |
Aparece en las colecciones: | (IIQ) Artículos |
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