Article
Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry
Author/s | 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 |
Publication Date | 2018 |
Deposit Date | 2019-01-25 |
Published in |
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Awards | Premio Mensual Publicación Científica Destacada de la US. Facultad de Química |
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 ... 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). |
Funding agencies | Ministerio de Economía y Competitividad (MINECO). España Junta de Andalucía |
Project ID. | CTQ2016-77270-R
FQM-345 |
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. |
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