| Título | Discovery of a Potent a-Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine-(Thio)urea Hybrid Molecules Generated via Click Chemistry |
|---|---|
| Autores | Elias-Rodriguez, Pilar , PINGITORE, VALERIA, Carmona, Ana T. , Moreno-Vargas, Antonio J. , Ide, Daisuke , Miyawaki, Shota , Kato, Atsushi , Alvarez, Eleuterio , Robina, Inmaculada |
| Publicación externa | Si |
| Medio | J. Org. Chem. |
| Alcance | Article |
| Naturaleza | Científica |
| Cuartil JCR | 1 |
| Cuartil SJR | 1 |
| Impacto JCR | 4.745 |
| Fecha de publicacion | 17/08/2018 |
| ISI | 000442451500006 |
| DOI | 10.1021/acs.joc.8b01073 |
| Abstract | The parallel synthesis of a 26-membered-library of aromatic/aliphatic-(thio)urea-linked pyrrolizidines followed by in situ biological evaluation toward alpha-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 alpha-galactosidase inhibitor (IC50 = 0.37 mu M, K-i = 0.12 mu M) that has also showed inhibition against human lysosomal alpha-galactosidase (alpha-Gal A, IC50 = 5.3 mu M, K-i = 4.2 mu M). |
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