首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and antidiabetic activity of 2,4-thiazolidindione, imidazolidinedione and 2-thioxo-imidazolidine-4-one derivatives bearing 6-methyl chromonyl pharmacophore
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Synthesis and antidiabetic activity of 2,4-thiazolidindione, imidazolidinedione and 2-thioxo-imidazolidine-4-one derivatives bearing 6-methyl chromonyl pharmacophore

机译:2,4-噻唑烷二酮,咪唑烷二酮和2-硫代-咪唑烷-4-酮衍生物的合成及其抗糖尿病活性

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摘要

Numerous compounds have been prepared in orderto improve the pharmacological profile of insulinotropic activities. !n the present paper, we report the synthesis and the in vitro insulin releasing activity of the 6-methyl-chromonyl-2,4-thiazolidinediones (Illa-c, IVa-c, Va-c). Compounds Mb, Ilk, IVa-c, Va and Vc (at lower concentration; 0.001 mg/mL) were able to increase insulin release in the presence of 5.6 mmol/L glucose. In this series, the most potent compound is IVa having methyl group at N3 position of TZD ring.
机译:为了改善促胰岛素活性的药理特性,已经制备了许多化合物。在本论文中,我们报告了6-甲基-苯甲酰基-2,4-噻唑烷二酮(IIIa-c,IVa-c,Va-c)的合成和体外胰岛素释放活性。化合物Mb,Ilk,IVa-c,Va和Vc(较低浓度; 0.001 mg / mL)在存在5.6 mmol / L葡萄糖的情况下能够增加胰岛素释放。在该系列中,最有效的化合物是在TZD环的N3位具有甲基的IVa。

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