Beilstein J. Org. Chem.2005,1, No. 12, doi:10.1186/1860-5397-1-12
, Laboratoire de Cristallographie et RMN Biologiques, 4 avenue de l'Observatoire, 75270 Paris Cedex 06, France 10.1186/1860-5397-1-12 Abstract Background
Glycosidases are involved in several metabolic pathways and the development of inhibitors is an important challenge towards the treatment of diseases, such
particular case, due to the hindered conformation of such epoxides as demonstrated by X-ray cristallographic analysis.
Conclusion
The biological activity of the synthesized glycomimetics has been evaluated towards 24 commercially available glycosidases. The weak observed activities can probably be related to
towards glycosidases, while the core structure and essential network of hydroxyl functionalities for enzyme recognition are retained. An important example is the 1-deoxynojirimycin (DNJ) family, for which DNJ itself is a competitive inhibitor of α-D-glucosidase (Ki = 8–25 μM),[10] while its derivatives
Beilstein J. Org. Chem.2005,1, No. 2, doi:10.1186/1860-5397-1-2
LS2 9JT, UK School of Chemistry, University of Leeds, Leeds LS2 9JT, UK 10.1186/1860-5397-1-2 Abstract Background
Many polyhydroxylated piperidines are inhibitors of the oligosaccharide processing enzymes, glycosidases and glycosyltransferases. Aza-C-linked disaccharide mimetics are compounds in
polyhydroxylated piperidines are potent inhibitors of the oligosaccharide processing enzymes, glycosidases and glycosyltransferases.[1][2][3] For example, deoxymannojirimycin, 1, and deoxynojirimycin, 2, are selective mannosidase and glucosidase inhibitors respectively.[4][5] In these molecules, the nitrogen atom