Exploring Multivalent Architectures for Binding and Stabilization of N-Acetylgalactosamine 6-Sulfatase [PDF]
MoleculesMorquio A syndrome is a lysosomal disorder caused by the deficiency of the lysosomal enzyme N-acetylgalactosamine 6-sulfatase (GALNS, EC 3.1.6.4).
Maria Giulia Davighi +8 more
doaj +2 more sources
Targeting N-Acetylglucosaminidase in Staphylococcus aureus with Iminosugar Inhibitors [PDF]
AntibioticsBacteria are capable of remarkable adaptations to their environment, including undesirable bacterial resistance to antibacterial agents. One of the most serious cases is an infection caused by multidrug-resistant Staphylococcus aureus, which has ...
Janja Sluga +9 more
doaj +2 more sources
A hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE) [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022 The synthesis of four heterodimers in which the copper(I)-catalysed azide-alkyne cycloaddition was employed to connect a 1-deoxynojirimycin moiety with a benzotriazole scaffold is reported.
Tereza Cristina Santos Evangelista +8 more
doaj +2 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
Crystal structure of 6-azido-6-deoxy-1,2-O-isopropylidene-α-d-glucofuranose
Acta Crystallographica Section E: Crystallographic Communications, 2020 Short syntheses to high Fsp3 index natural-product analogues such as iminosugars are of paramount importance in the investigation of their biological activities and reducing the use of protecting groups is an advantageous synthetic strategy.
Adam Wood +3 more
doaj +1 more source
Molecules, 2022 A series of N-substituted iminosugar C-glycosides were synthesized and tested for α-glucosidase inhibition. The results suggested that 6e is a promising and potent α-glucosidase inhibitor.
Haibo Wang +5 more
doaj +1 more source
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
Molecules, 2022 Bambusurils, BU[4] and BU[6], were used for the first time as multivalent scaffolds to link glycosidases inhibitors derived from 1-deoxynojirimycin (DNJ).
Marine Lafosse +6 more
doaj +1 more source
Synthesis of Piperidine Nucleosides as Conformationally Restricted Immucillin Mimics
Molecules, 2021 The de novo synthesis of piperidine nucleosides from our homologating agent 5,6-dihydro-1,4-dithiin is herein reported. The structure and conformation of nucleosides were conceived to faithfully resemble the well-known nucleoside drugs Immucillins H and ...
Maria De Fenza +3 more
doaj +1 more source