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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones.
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Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones.

机译：一些新的苯二甲酰基-2,4-噻唑烷二酮的合成及醛糖还原酶抑制活性。

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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 chromonyl-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 Ia-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).
机译：众所周知，市场上还没有任何自信的ARI，并且它们具有多种副作用，我们需要批准新的ARI以减少糖尿病并发症，尤其是对白内障形成有影响的糖尿病。在这项研究中，通过Knoevenagel反应与取代的3-甲酰基色酮（3a-e）和未取代的（1）或取代的取代基制备了一系列新的苯甲酰基-2,4-噻唑烷二酮（Ia-e，IIa-e，IIIa-e） 2,4-噻唑烷二酮（2）。通过体外分光光度法测试合成的化合物抑制大鼠肾脏AR的能力。化合物IIIe显示出最高的抑制活性（82.43 +/- 0.76％）。化合物Ia-e和IIIa-d也显示出显着的抑制活性（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％）。

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