Dipartimento di Chimica G. Ciamician, Università di Bologna, Via Selmi 2, I-40126 Bologna.
Chem Biodivers. 2010 Jan;7(1):225-8. doi: 10.1002/cbdv.200900096.
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.
研究了一系列手性哌嗪-2,5-二酮衍生物对α-和β-葡萄糖苷酶的抑制潜力。在所测试的七种化合物中，有三种，即 1、5b 和 5c，被证明是非竞争性α-葡萄糖苷酶抑制剂，而它们对β-葡萄糖苷酶的抑制活性很低。最活跃的化合物 5c（α-葡萄糖苷酶的 K（I）=5 微米）对α-葡萄糖苷酶/β-葡萄糖苷酶抑制剂的选择性有 100 倍。
