Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Tamilnadu, India.
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1953-6. doi: 10.1016/j.bmcl.2010.01.125. Epub 2010 Feb 1.
Glitazones are known to exhibit antihyperglycemic activity by decreasing peripheral insulin resistance. In the present study, we have designed some novel glitazones based on the structure-activity relationships as possible PPAR-gamma agonists. The manually designed glitazones were synthesized by using the appropriate synthetic schemes and screened for their in vitro antihyperglycemic activity by estimating glucose uptake by rat hemi-diaphragm, both in the absence and in the presence of external insulin. Some of the glitazones exhibited good antihyperglycemic activity in presence of insulin. Illustration about their design, synthesis, evaluation, and structure-activity relationships is described.
噻唑烷二酮类药物通过降低外周胰岛素抵抗来表现出抗高血糖活性。在本研究中，我们根据构效关系设计了一些新的噻唑烷二酮类药物，作为潜在的过氧化物酶体增殖物激活受体-γ激动剂。通过估计大鼠半膈肌的葡萄糖摄取，在手性设计的噻唑烷二酮类药物的基础上，使用适当的合成方案进行合成，并在存在和不存在外源性胰岛素的情况下对其进行体外抗高血糖活性筛选。一些噻唑烷二酮类药物在胰岛素存在的情况下表现出良好的抗高血糖活性。描述了它们的设计、合成、评估和构效关系。
