Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones

被引:37
作者
Bozdak-Dundar, Oya [1 ]
Evranos, Begiim [1 ]
Das-Evcimen, Net [2 ]
Sarikaya, Mutlu [2 ]
Ertan, Rahmiye [1 ]
机构
[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Ankara Univ, Fac Pharm, Dept Biochem, TR-06100 Ankara, Turkey
关键词
Chromone derivatives; 2,4-Thiazolidinediones; Chromonyl-2,4-thiazolidinediones; Aldose reductase; Aldose reductase inhibition; Synthesis;
D O I
10.1016/j.ejmech.2008.01.004
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
As it is known that still, there were no any confident ARIs on the market and they have several side effects, we need to approve new ARIs to reduce diabetic complications especially which have effect on the cataract formation. In this study, a new series of chromonl-2,4-thiazolidinediones (Ia-e, IIa-e, IIIa-e) were prepared by Knoevenagel reaction with substituted 3-formylchromones (3a-e) and unsubstituted (1) or substituted 2,4-thiazolidinedione (2). The synthesized compounds were tested for their ability to inhibit rat kidney AR by an in vitro spectrophotometric assay. Compound IIIe showed the highest inhibitory activity (82.43 +/- 0.76%). Compounds la-e and IIIa-d also showed significant inhibitory activity (42.40 +/- 5.78, 52.71 +/- 3.31, 49.69 +/- 1.55, 50.80 +/- 3.62, 46.70 +/- 2.33, 49.44 +/- 4.53, 61.17 +/- 4.74, 68.58 +/- 2.05, 77.28 +/- 0.26%, respectively). (C) 2008 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:2412 / 2417
页数:6
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