Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Rocklands, Ootacamund 643 001, India.
Eur J Med Chem. 2011 Mar;46(3):835-44. doi: 10.1016/j.ejmech.2010.12.019. Epub 2010 Dec 23.
Three series of novel glitazones were designed and prepared by using appropriate synthetic schemes to incorporate glycine, aromatic and alicyclic amines via two carbon linker. Compounds were synthesized both under conventional and microwave methods. Nineteen out of twenty four synthesized compounds were evaluated for their in vitro glucose uptake activity using isolated rat hemi-diaphragm. Compounds, 6, 9a, 13a, 13b, 13c, 13f and 13h exhibited significant glucose uptake activity. Illustration about their synthesis and in vitro glucose uptake activity is described along with the structure-activity relationships.
设计并合成了三系列新型噻唑烷二酮类化合物,通过两个碳连接链将甘氨酸、芳香族和脂环族胺引入其中。化合物采用常规法和微波法进行合成。采用离体大鼠膈肌法,对 24 个合成化合物中的 19 个进行了体外葡萄糖摄取活性评价。化合物 6、9a、13a、13b、13c、13f 和 13h 表现出显著的葡萄糖摄取活性。本文描述了它们的合成及体外葡萄糖摄取活性的关系,并给出了结构-活性关系的说明。