Chiral Piperazine-2,5-dione Derivatives as Effective alpha-Glucosidase Inhibitors Part 4

The potential to inhibit alpha- and beta-glucosidases of a series of chiral piperazine-2,5-dione derivatives was investigated. Three of the seven compounds tested, viz., 1, 5b, and 5c, showed to be non competitive inhibitors of alpha-glucosidase, whereas they exhibited very low inhibitory activity towards beta-glucosidase. The most active compound, 5c (K(1) of alpha-glucosidase = 5 mu M), had a 100-fold alpha-glucosidase/beta-glucosidase inhibitor selectivity.