Beta-D-glycosylamidines: potent, selective, and easily accessible 1-glycosidase inhibitors

Beta-D-glycosylamidines, in which a glycon is connected via an N-glycoside linkage with a substituted amidine (aglycon), were synthesized in two steps from the corresponding sugars and served as stable and potent beta-glycosidase inhibitors with high selectivity according to the glycon- and alpha, beta-specificities of the enzymes.