Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandogan, Ankara, Turkey.
J Enzyme Inhib Med Chem. 2012 Jun;27(3):419-27. doi: 10.3109/14756366.2011.594047. Epub 2011 Jul 8.
We report the synthesis and the in vitro insulin releasing and glucose uptake activity of the morpholino thiazolyl-2,4-thiazolidinediones (1-15). Compounds 5, 11-15 (at lower concentration; 0.001 mg/ml) were able to increase insulin release in the presence of 5.6 mmol/l glucose. The compounds, except derivative 3 show an increase of glucose uptake. Various compounds are interesting potential antidiabetic leads showing pancreatic and extrapancreatic effects.
我们报告了吗啉噻唑基-2,4-噻唑烷二酮(1-15)的合成及体外胰岛素释放和葡萄糖摄取活性。化合物 5、11-15(浓度较低;0.001 mg/ml)能够在 5.6 mmol/l 葡萄糖存在的情况下增加胰岛素释放。除了衍生物 3 之外,这些化合物都显示出葡萄糖摄取的增加。各种化合物都是有潜力的抗糖尿病先导化合物,具有胰腺和胰外作用。