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Artículo
Pharmacological chaperone therapy for Gaucher disease: A patent review
(Taylor & Francis, 2011)
Introduction: Mutations in the gene encoding for acid β-glucosidase (β-glucocerebrosidase, GlcCerase) are seen in Gaucher disease (GD), which give rise to significant protein misfolding effects and result in progressive ...
Artículo
Tuning the activity of iminosugars: novel N-alkylated deoxynojirimycin derivatives as strong BuChE inhibitors
(Taylor & Francis Open Access, 2021)
We have designed unprecedented cholinesterase inhibitors based on 1-deoxynojirimycin as potential anti-Alzheimer’s agents. Compounds are comprised of three key structural motifs: the iminosugar, for interaction with ...
Artículo
Syntheses and biological activities of 1,4-iminoalditol derivatives as α-L-fucosidase inhibitors
(Schweizerische Chemische Gesellschaft (Swiss Chemistry Society), 2011)
A review dealing with 1,4-iminoalditol (hydroxylated pyrrolidine) derivatives as inhibitors of α-l-fucosidases including the different synthetic approaches for their preparation as well as their inhibitory properties is presented.
Artículo
Preparation of water-soluble glycopolymers derived from five-membered iminosugars
(Elsevier, 2019-10)
Iminosugars are carbohydrate mimetics that constitute the main group of oligosaccharide processing enzyme inhibitors. They play an important role in cell-cell recognition processes, thereby presenting a wide range ...
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 ...
Artículo
Mechanistic Insight into the Binding of Multivalent Pyrrolidines to α-Mannosidases
(Wiley-Blackwell, 2017)
Novel pyrrolidine-based multivalent iminosugars, synthesized by a CuAAC approach, have shown remarkable multivalent effects towards jack bean α-mannosidase and a Golgi α-mannosidase from Drosophila melanogaster, as well ...
Artículo
Structural Basis of the Inhibition of GH1 β-glucosidases by Multivalent Pyrrolidine Iminosugars
(Elsevier, 2019)
The synthesis of multivalent pyrrolidine iminosugars via CuAAC click reaction between different pyrrolidine-azide derivatives and tri- or hexavalent alkynyl scaffolds is reported. The new multimeric compounds, together ...
Artículo
Stereoselective Synthesis of Iminosugar 2-Deoxy(thio)glycosides from Bicyclic Iminoglycal Carbamates Promoted by Cerium(IV) Ammonium Nitrate and Cooperative Brønsted Acid-Type Organocatalysis
(American Chemical Society, 2020)
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 ...
Artículo
Discovery of human hexosaminidase inhibitors by in situ screening of a library of mono- and divalent pyrrolidine iminosugars
(Elsevier, 2022)
Two libraries of mono- and dimeric pyrrolidine iminosugars were synthesized by CuAAC and (thio)urea-bond-forming reactions from the respective azido/aminohexylpyrrolidine iminosugar precursors. The resulting monomeric and ...