El trabajo realizado durante el desarrollo del ciclo de mejora experimentado en la asignatura Experimentación en Química II se ha centrado en dos pilares fundamentales: 1) Interconexión de los contenidos teórico-prácticos de modo que el conocimiento que se construya sea un conocimiento con cimientos sólidos, constituido por experiencias que se...
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May 15, 2019 (v1)PublicationUploaded on: December 2, 2022
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May 27, 2022 (v1)Publication
Lysosomal storage disorders (LSDs) are often caused by mutations that destabilize native folding and impair the trafficking of enzymes, leading to premature endoplasmic reticulum (ER)-associated degradation, deficiencies of specific hydrolytic functions and aberrant storage of metabolites in the lysosomes. Enzyme replacement therapy (ERT) and...
Uploaded on: March 25, 2023 -
November 4, 2022 (v1)Publication
Derivados sp2 imnoazúcar como inhibidores de las ?-glicosidasas.Derivados glicosilados de fórmula I, donde los significados para los distintos sustituyentes son los indicados en la descripción. Estos compuestos son útiles como inhibidores de las ?-glicosi
Uploaded on: March 24, 2023 -
April 7, 2017 (v1)Publication
sp2-Iminosugar-type castanospermine analogues have been shown to exhibit anti-tumor activity. However, their effects on cell proliferation and apoptosis and the molecular mechanism at play are not fully understood. Here, we investigated the effect of two representatives, namely the pseudo-S- and C-octyl glycoside 2-oxa-3-oxocastanospermine...
Uploaded on: December 5, 2022 -
November 30, 2022 (v1)Publication
The first examples of iminosugar-type 2-deoxy(thio)glycoside mimetics are reported. The key step is the activation of a bicyclic iminoglycal carbamate to generate a highly reactive acyliminium cation. Cerium(IV) ammonium nitrate efficiently promoted the formation of 2-deoxy S-glycosides in the presence of thiols, probably by in situ generation...
Uploaded on: March 24, 2023 -
April 8, 2021 (v1)Publication
Diabetic retinopathy (DR) is one of the most common complications of Diabetes Mellitus (DM) and is directly associated with inflammatory processes. Currently, neuro-inflammation is considered an early event in DR and proceeds via microglia polarization. A hallmark of DR is the presence of retinal reactive gliosis. Here we report the beneficial...
Uploaded on: December 4, 2022 -
October 16, 2019 (v1)PublicationThiol-ene "Click" Synthesis and Pharmacological Evaluation of C-Glycoside sp2-Iminosugar Glycolipids
The unique stereoelectronic properties of sp2-iminosugars enable their participation in glycosylation reactions, thereby behaving as true carbohydrate chemical mimics. Among sp2-iminosugar conjugates, the sp2-iminosugar glycolipids (sp2-IGLs) have shown a variety of interesting pharmacological properties ranging from glycosidase inhibition to...
Uploaded on: March 25, 2023 -
January 28, 2022 (v1)Publication
sp2-Iminosugar glycolipids (sp2-IGLs) represent a consolidated family of glycoconjugate mimetics encompassing a monosaccharide-like glycone moiety with a pseudoamide-type nitrogen replacing the endocyclic oxygen atom of carbohydrates and an axially-oriented lipid chain anchored at the pseudoanomeric position. The combination of these structural...
Uploaded on: March 25, 2023 -
July 18, 2018 (v1)Publication
A series of conformationally locked C-glycosides based on the 3-aminopyrano[3,2-b]pyrrol-2(1H)-one (APP) scaffold has been synthesized. The key step involved a totally stereocontrolled C-Michael addition of a serine-equivalent C-nucleophile to tri-O-benzyl-2-nitro-D-galactal, previously published by the authors. Stereoselective transformations...
Uploaded on: March 27, 2023 -
September 19, 2018 (v1)Publication
A series of sp2-iminosugar-type glycomimetics bearing S-linked pseudoglycoside substituents (sulfide, sulfoxide and sulfone derivatives) has been synthesized and evaluated as new potential drugs against the protozoan parasite Leishmania, responsible of leishmaniasis, the second most relevant parasitic disease after malaria. All the prepared...
Uploaded on: March 27, 2023 -
May 10, 2023 (v1)Publication
The unique electronic properties of the fluorine atom make its strategic incorporation into a bioactive compound a very useful tool in the design of drugs with optimized pharmacological properties. In the field of the carbo- hydrates, its selective installation at C2 position has proven particularly interesting, some...
Uploaded on: May 11, 2023 -
March 10, 2022 (v1)Publication
The Tn antigen (GalNAc-α-1-O-Thr/Ser) is a well-known tumor-associated carbohydrate determinant. The use of glycopeptides that incorporate this structure has become a significant and promising niche of research owing to their potential use as anticancer vaccines. Herein, the conformational preferences of a glycopeptide with an unnatural Tn...
Uploaded on: December 5, 2022 -
December 15, 2022 (v1)Publication
Glycolipid mimetics consisting of a bicyclic polyhydroxypiperidine-cyclic carbamate core and a pseudoanomeric hydrophobic tail, termed sp2-iminosugar glycolipids (sp2-IGLs), target microglia during neuroinflammatory processes. Here we have synthesized and investigated new variants of sp2-IGLs for their ability to suppress the activation of...
Uploaded on: March 24, 2023 -
May 18, 2018 (v1)Publication
Amphiphilic glycomimetics encompassing a rigid, undistortable nor-tropane skeleton based on 1,6-anhydro-L-idonojirimycin and a polyfluorinated antenna, when formulated as the corresponding inclusion complexes with β-cyclodextrin (βCD), have been shown to behave as pharmacological chaperones (PCs) that efficiently rescue lysosomal β-...
Uploaded on: March 26, 2023 -
July 11, 2024 (v1)Publication
Background: The number of patients treated with coagulation disorders, and more specifically with anticoagulant therapy, has increased worldwide in recent years due to increased life expectancy in developed countries. The protocols for managing this type of patient in oral surgery has varied over recent years, especially after the appear ance...
Uploaded on: July 12, 2024 -
September 2, 2022 (v1)Publication
Inflammatory processes play a central role in the pathogenesis of diabetic nephropathy (DN) in the early stages of the disease. The authors demonstrate that the glycolipid mimetic (Ss)-DS-ONJ is able to abolish inflammation via the induction of autophagy flux and provokes the inhibition of inflammasome complex in ex vivo and in vitro models,...
Uploaded on: March 25, 2023