Glycosidase Inhibitors

Carbohydrate analogues with basic nitrogen instead of oxygen in the sugar ring have become one of the most important classes of competitive glycosidase inhibitors during the last decade. Because of the strong interaction with a large variety of metabolic processes many compounds have interesting biological properties. Anti-retroviral, antimetastatic, immune stimulating, antirheumatic, antidiabetic and in some cases antibacterial activities have also been found. Quite a few of these imino sugars are already on the market (migitolâ) or in the last stage of clinical studies. Our group is engaged in the synthesis and chemical modification of some of these glycosidase inhibitors as well as in close co-operation with an international team of groups for example from the University of British Columbia, Vancouver, from CSIRO, Melbourne, and from the Technical University of Denmark, Lyngby-Copenhagen - with the biological evaluation of these products. With the aid of computer supported molecular modeling studies and in collaboration with internationally leading crystallographers, the interactions of some of these compounds with the active site of selected enzymes can be explored to gain increasing information on the structure-activity-relationships in this class of inhibitors.