In vitro comparison of the glycosidase inhibitory profile of isoiminosugars with their 1- and 5a-modified derivatives.

Isoiminosugars are a group of glycomimetics known for being among the most potent glycosidase inhibitors, making them attractive as lead compounds in drug discovery. This review article summarizes how glycosidase inhibitory activities in in vitro assays are influenced by substituents attached to the 1- and 5a-positions of polyhydroxylated piperidine isoiminosugars, compared to their non-substituted parent compounds. Additionally, the review gives an overview of the glycosidase inhibitory properties of common iminosugars. It also discusses how these properties are affected when the nitrogen atom in iminosugars, which occupies the position of the endocyclic oxygen atom in monosaccharides, is relocated to the position of the anomeric carbon atom to form isoiminosugars.