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Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry

 

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Opened Access Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry
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Author: Elías Rodríguez, María del Pilar
Pingitore, Valeria
Carmona Asenjo, Ana Teresa
Moreno Vargas, Antonio José
Ide, Daisuke
Miyawaki, Shota
Kato, Atsushi
Álvarez González, Eleuterio
Robina Ramírez, Inmaculada
Department: Universidad de Sevilla. Departamento de Química orgánica
Date: 2018
Published in: The Journal of Organic Chemistry, 83, 8863-8873.
Document type: Article
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).
Cite: 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.
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URI: https://hdl.handle.net/11441/82051

DOI: 10.1021/acs.joc.8b01073

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