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Mostrando ítems 1-10 de 27
Artículo
Stable Pyrrole-Linked Bioconjugates through Tetrazine-Triggered Azanorbornadiene Fragmentation
(Wiley-Blackwell, 2020)
An azanorbornadiene bromovinyl sulfone reagent for cysteine-selective bioconjugation has been developed. Subsequent reaction with dipyridyl tetrazine leads to bond cleavage and formation of a pyrrole-linked conjugate. The ...
Artículo
Synthesis and Biological Evaluation of Modified 2-Deoxystreptamine Dimers
(Thieme Publishing; Georg Thieme Verlag, 2011)
Aminoglycosides are powerful antibiotics, but the emergence of resistant bacterial strains has prompted the search for analogues with better pharmacological profiles. The synthesis of 2-deoxystreptamine (2-DOS) dimers ...
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 ...
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
Synthesis and Structure-activity Relationship of New Nicotinamide Phosphoribosyltransferase Inhibitors with Antitumor Activity on Solid and Haematological Cancer
(Elsevier, 2023)
Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT) activity for proliferation, therefore NAMPT represents an interesting target for the development of anti-cancer drugs. Several compounds, ...
Artículo
Transferring Substituents from Alkynes to Furans and Pyrroles through Heteronorbornadienes as Intermediates: Synthesis of β-Substituted Pyrroles/Furans
(American Chemical Society, 2023)
The use of 7-oxa/azanorbornadienes as synthetic intermediates for the preparation of 3/4-substituted (β-substituted) furans/pyrroles is presented. The method lies in the inverse electron demand Diels-Alder (iEDDA) cycloaddition ...
Artículo
Synthesis of Novel 3-Amino(Hydroxy)methyl-l-fuco-Azafagomines as Leads for Selective Inhibitors of α-l-Fucosidases
(2010)
The synthesis of 3-substituted l-fuco-azafagomines from d-lyxose is reported. They represent the first example of aza-C-glycosides having a biimino (-NH-NH-) moiety. The key step of the synthesis is the introduction of the ...
Artículo
Total asymmetric synthesis of monosaccharides and analogues
(Schweizerische Chemische Gesellschaft (Swiss Chemistry Society), 2011)
Since the discovery of the 'formose reaction' by Butlerow,[1] total synthesis of carbohydrates has undergone rapid development. The most important methods for the asymmetric synthesis of monosaccharides and analogues of ...
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 ...