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(I) of alpha-glucosidase=5 microm), had a 100-fold alpha-glucosidase/beta-glucosidase inhibitor selectivity.
Arcelli
Antonio
A
Dipartimento di Chimica G. Ciamician, Università di Bologna, Via Selmi 2, I-40126 Bologna. antonio.arcelli@unibo.it
Balducci
Daniele
D
Porzi
Gianni
G
Sandri
Monica
M
D001667:Binding, Competitive; D044602:Cellulases / Q000037:antagonists & inhibitors / Q000378:metabolism; D054659:Diketopiperazines / Q000138:chemical synthesis / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D065089:Glycoside Hydrolase Inhibitors; D013237:Stereoisomerism; D000520:alpha-Glucosidases / Q000378:metabolism
D054659:Diketopiperazines; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D044602:Cellulases; D000520:alpha-Glucosidases