Artículos (Química Orgánica)

URI permanente para esta colecciónhttps://hdl.handle.net/11441/10924

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Examinando Artículos (Química Orgánica) por Premio "Premio Mensual Publicación Científica Destacada de la US. Facultad de Química"

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    Acceso AbiertoPremio Mensual Publicación Científica Destacada de la US. Facultad de QuímicaArtículo
    Bifunctional Squaramide Organocatalysts for the Asymmetric Addition of Formaldehyde tert-Butylhydrazone to Simple Aldehydes
    (Wiley-Blackwell, 2018) Matador Martínez, Esteban; de Gracia Retamosa, María; Monge Fernández, David; Iglesias Sigüenza, Francisco Javier; Fernández Fernández, Rosario Fátima; Lassaletta, José M.; Universidad de Sevilla. Departamento de Química orgánica; Ministerio de Economía y Competitividad (MINECO). España; Junta de Andalucía
    The nucleophilic addition of formaldehyde tert-butylhydrazone to simple aldehydes (a formal hetero-carbonyl–ene reaction) can be performed with good reactivity and excellent enantioselectivity by virtue of the dual hydrogen-bonding activation exerted by amide–squaramide organocatalysts. The resulting hydroxydiazenes (azo alcohols) were isolated in high yields as enantiomerically enriched azoxy compounds after a regioselective azo-to-azoxy transformation. Subsequent derivatization provides an entry to relevant amino alcohols, oxazolidinones, and derivatives thereof.
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    Acceso AbiertoPremio Mensual Publicación Científica Destacada de la US. Facultad de QuímicaArtículo
    Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry
    (American Chemical Society, 2018) 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; Universidad de Sevilla. Departamento de Química orgánica; Ministerio de Economía y Competitividad (MINECO). España; Junta de Andalucía
    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).