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

被引：3

作者：

Arcelli, Antonio ^{[1
]}

Balducci, Daniele ^{[2
]}

Porzi, Gianni ^{[1
]}

Sandri, Monica ^{[3
]}

机构：

[1] Univ Bologna, Dipartimento Chim G Ciamician, I-40126 Bologna, Italy

[2] Univ Coll Dublin, Sch Chem & Chem Biol, Belfield 4, Irl Dublin, Ireland

[3] CNR, ISTEC, I-48018 Faenza, Italy

来源：

CHEMISTRY & BIODIVERSITY | 2010年 / 7卷 / 01期

关键词：

1,4-MORPHOLIN-2,5-DIONE DERIVATIVES; ANALOGS;

D O I：

10.1002/cbdv.200900096

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：225 / 228

页数：4

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