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Artículo
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
(Taylor & Francis, 2022)
Herein, we report the preparation of a panel of Schiff bases analogues as antiprotozoal agents by modification of the stereoelectronic effects of the substituents on N-1 and N-4 and the nature of the chalcogen atom (S, ...
Artículo
sp2-Iminosugars targeting human lysosomal β-hexosaminidase as pharmacological chaperone candidates for late-onset Tay-Sachs disease
(Taylor & Francis, 2022)
The late-onset form of Tay-Sachs disease displays when the activity levels of human β-hexosaminidase A (HexA) fall below 10% of normal, due to mutations that destabilise the native folded form of the enzyme and impair its ...
Artículo
Tackling Antibiotic Resistance: Influence of Aliphatic Branches on Broad-Spectrum Antibacterial Polytriazoles against ESKAPE Group Pathogens
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
One of the most important threats to public health is the appearance of multidrug-resistant pathogenic bacteria, since they are the cause of a high number of deaths worldwide. Consequently, the preparation of new effective ...
Artículo
Iridium-and Palladium-Based Catalysts in the Pharmaceutical Industry
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
Transition metal catalysts play a vital role in a wide range of industrial organic processes. The large-scale production of chemicals relying on catalyzed organic reactions represents a sustainable approach to supply society ...
Artículo
Inter-Ligand STD NMR: An Efficient 1D NMR Approach to Probe Relative Orientation of Ligands in a Multi-Subsite Protein Binding Pocket
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
In recent years, Saturation Transfer Difference NMR (STD NMR) has been proven to be a powerful and versatile ligand-based NMR technique to elucidate crucial aspects in the investigation of protein-ligand complexes. Novel ...
Tesis Doctoral
Nuevos tio- y selenoderivados de carbohidratos en enfermedades degenerativas: cáncer y Alzheimer
(2022-07-08)
En la presente Tesis Doctoral se han desarrollado nuevas familias de compuestos bioactivos frente a enfermedades complejas y multifactoriales, como son el cáncer y el Alzheimer. Gran parte de la investigación ha estado ...
Artículo
Chemoselective Preparation of New Families of Phenolic-Organoselenium Hybrids—A Biological Assessment
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
Being aware of the enormous biological potential of organoselenium and polyphenolic compounds, we have accomplished the preparation of novel hybrids, combining both pharma-cophores in order to obtain new antioxidant and ...
Artículo
Squaramide-Tethered Sulfonamides and Coumarins: Synthesis, Inhibition of Tumor-Associated CAs IX and XII and Docking Simulations
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
(1) Background: carbonic anhydrases (CAs) are attractive targets for the development of new anticancer therapies; in particular, CAs IX and XII isoforms are overexpressed in numerous tumors. (2) Methods: following the tail ...
Artículo
Biocatalytic Atroposelective Synthesis of Axially Chiral N-Arylindoles via Dynamic Kinetic Resolution
(American Chemical Society, 2022-12-22)
A highly enantioselective biocatalytic dynamic kinetic resolution (DKR) of configurationally labile N-arylindole aldehydes is described. The DKR proceeds by atroposelective bioreduction of the carbonyl group catalyzed by ...
Artículo
A hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE).
(Taylor and Francis Group, 2022)
The synthesis of four heterodimers in which the copper(I)-catalysed azide-alkyne cycloaddition wasemployed to connect a 1-deoxynojirimycin moiety with a benzotriazole scaffold is reported. The hetero-dimers were investigated ...