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一些新的色烯基-2,4-噻唑烷二酮的合成及抗糖尿病活性。

Synthesis and antidiabetic activity of some new chromonyl-2,4-thiazolidinediones.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandoğan, Ankara, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2010 Dec;25(6):784-9. doi: 10.3109/14756360903357544. Epub 2010 Aug 5.

DOI:10.3109/14756360903357544
PMID:20687791
Abstract

A series of chromonyl-2,4-thiazolidinediones/imidazolidinediones/2-thioxo-imidazolidine-4-ones (IIIa-i, IVa-i) was prepared by Knoevenagel reaction of 2,4-thiazolidinedione/2,4-imidazolidinedione/2-thioxo-imidazolidine-4-one (IIa-c) with 2/3-formyl chromone (Ia-b) and then alkylation with methyl/ethyl iodide. The prepared compounds were tested for their insulinotropic activities in INS-1 cells. Compounds ıVb and ıVc (at lower concentration, 1 μg/mL) were able to increase insulin release in the presence of 5.6 mmol/L glucose." should be written as "Compounds IVb and IVc (at lower concentration, 1 µg/mL) and also IIId and IIIg (at higher concentration) were able to increase insulin release in the presence of 5.6 mmol/L glucose. Compounds ıVb and ıVc (at lower concentration, 1 μg/mL) were able to increase insulin release in the presence of 5.6 mmol/L glucose.

摘要

一系列的色原酮-2,4-噻唑烷二酮/咪唑烷二酮/2-硫代咪唑烷-4-酮(IIIa-i,IVa-i)通过 2,4-噻唑烷二酮/2,4-咪唑烷二酮/2-硫代咪唑烷-4-酮(IIa-c)与 2/3-甲酰基色酮(Ia-b)的 Knoevenagel 反应,然后与碘甲烷/碘乙烷进行烷基化反应制备得到。所制备的化合物在 INS-1 细胞中进行了胰岛素促分泌活性测试。化合物 IVb 和 IVc(在较低浓度,1μg/mL)在 5.6mmol/L 葡萄糖存在的情况下能够增加胰岛素的释放。"

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