Multivalent Pyrrolidine Iminosugars: Synthesis and Biological Relevance
Molecules, 2022 Recently, the strategy of multivalency has been widely employed to design glycosidase inhibitors, as glycomimetic clusters often induce marked enzyme inhibition relative to monovalent analogs.
Yali Wang +3 more
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Synthesis of pyrrolidine-based hamamelitannin analogues as quorum sensing inhibitors in Staphylococcus aureus [PDF]
Beilstein Journal of Organic Chemistry, 2018 Interfering with bacterial cell-to-cell communication is a promising strategy to combat antimicrobial resistance. The natural product hamamelitannin and several of its analogues have been identified as quorum sensing inhibitors.
Jakob Bouton +3 more
doaj +2 more sources
Exploring architectures displaying multimeric presentations of a trihydroxypiperidine iminosugar [PDF]
Beilstein Journal of Organic Chemistry, 2015 The synthesis of new multivalent architectures based on a trihydroxypiperidine α-fucosidase inhibitor is reported herein. Tetravalent and nonavalent dendrimers were obtained by means of the click chemistry approach involving the copper azide-alkyne ...
Camilla Matassini +5 more
doaj +6 more sources
Simultaneous Grafting of 3,4,5-Trihydroxypiperidine Iminosugars Onto Multivalent Scaffolds via Double Reductive Amination Provides New GCase Inhibitors. [PDF]
ChemistryA small set of low‐valency multivalent 3,4,5‐trihydroxypiperidines was prepared through double reductive amination (DRA) of a sugar‐derived dialdehyde. Among them, trivalent derivative 37 emerged as a potent β‐glucocerebrosidase (GCase) inhibitor displaying an unexpected mixed‐type kinetic profile. The integration of kinetic analysis, NMR, docking, and
Davighi MG +10 more
europepmc +2 more sources
New Castanospermine Glycoside Analogues Inhibit Breast Cancer Cell Proliferation and Induce Apoptosis without Affecting Normal Cells [PDF]
, 2013 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
Ahidouch, Ahmed +6 more
core +20 more sources
The Race to Salvage Glucocerebrosidase: Understanding Small-Molecule Therapies for GBA1-Associated Parkinsonism. [PDF]
Mov DisordVariants in GBA1, the gene encoding the lysosomal enzyme glucocerebrosidase, cause Gaucher disease and confer an increased risk for parkinsonism. Strategies using small molecules can improve the function of glucocerebrosidase in lysosomes. A clear understanding of the mechanism‐of‐action of these compounds will facilitate development of GBA1‐modulating
Henderson MJ +5 more
europepmc +2 more sources
A General Synthesis of Iminosugars. [PDF]
ChemInform, 2004 AbstractFor Abstract see ChemInform Abstract in Full Text.
Ciaran, McDonnell +3 more
openaire +2 more sources
Frontiers in Microbiology, 2020 Zika virus (ZIKV), a vector-borne virus of the family Flaviviridae, continues to spread and remains a significant global public health threat. Currently, there are no approved vaccines or antivirals against ZIKV.
Gitanjali Bhushan +5 more
doaj +1 more source
Beilstein Journal of Organic Chemistry, 2023 A synthesis of 1,4-imino-ᴅ-lyxitols and their N-arylalkyl derivatives altered at C-5 is reported. Their inhibitory activity and selectivity toward four GH38 α-mannosidases (two Golgi types: GMIIb from Drosophila melanogaster and AMAN-2 from ...
Martin Kalník +4 more
doaj +1 more source
Iminosugars: Promising therapeutics for influenza infection [PDF]
Critical Reviews in Microbiology, 2016 Influenza virus causes three to five million severe respiratory infections per year in seasonal epidemics, and sporadic pandemics, three of which occurred in the twentieth century and are a continuing global threat. Currently licensed antivirals exclusively target the viral neuraminidase or M2 ion channel, and emerging drug resistance necessitates the ...
Beatrice Ellen Tyrrell +4 more
openaire +2 more sources