Bozdağ-Dündar Oya, Verspohl Eugen J, Daş-Evcimen Net, Kaup Rebecca M, Bauer Katrin, Sarikaya Mutlu, Evranos Begüm, Ertan Rahmiye
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandoğan, Ankara, Turkey.
Bioorg Med Chem. 2008 Jul 15;16(14):6747-51. doi: 10.1016/j.bmc.2008.05.059. Epub 2008 Jun 17.
A new series of flavonyl-2,4-thiazolidinediones (Va-c, VIa-c) was prepared by Knoevenagel reaction. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR) and for their insulinotropic activities in INS-1 cells. Compound Vb was able to increase insulin release in the presence of 5.6mmol/l glucose. Compounds VIa-c displayed moderate to high AR inhibitory activity levels. Particularly, compound VIa showed the highest AR inhibitory activity (86.57%).
通过克诺文纳格尔反应制备了一系列新的黄酮基-2,4-噻唑烷二酮（Va-c，VIa-c）。对合成的化合物进行了抑制大鼠肾脏醛糖还原酶（AR）的能力以及在INS-1细胞中的促胰岛素活性测试。化合物Vb在5.6mmol/l葡萄糖存在下能够增加胰岛素释放。化合物VIa-c表现出中度至高的AR抑制活性水平。特别是，化合物VIa显示出最高的AR抑制活性（86.57%）。
