Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore 570 015, India.
Bioorg Chem. 2012 Dec;45:12-28. doi: 10.1016/j.bioorg.2012.08.002. Epub 2012 Aug 23.
We report a series of new glitazones incorporated with phenylalanine and tyrosine. All the compounds were tested for their in vitro glucose uptake activity using rat-hemidiaphragm, both in presence and absence of insulin. Six of the most active compounds from the in vitro screening were taken forward for their in vivo triglyceride and glucose lowering activity against dexamethazone induced hyperlipidemia and insulin resistance in Wistar rats. The liver samples of rats that received the most active compounds, 23 and 24, in the in vivo studies, were subjected to histopathological examination to assess their short term hepatotoxicity. The investigations on the in vitro glucose uptake, in vivo triglyceride and glucose lowering activity are described here along with the quantitative structure-activity relationships.
我们报告了一系列新的含苯丙氨酸和酪氨酸的噻唑烷二酮类化合物。所有化合物均采用大鼠膈肌在有胰岛素和无胰岛素的情况下进行体外葡萄糖摄取活性测试。从体外筛选中选出 6 种最活跃的化合物，用于研究它们对 Wistar 大鼠地塞米松诱导的高脂血症和胰岛素抵抗的体内降低甘油三酯和血糖的活性。在体内研究中接受最活跃的化合物 23 和 24 的大鼠的肝样本来进行组织病理学检查，以评估其短期肝毒性。本文还描述了体外葡萄糖摄取、体内降低甘油三酯和血糖活性的研究以及定量构效关系。
