5-(2-烷基/芳基-6-芳基咪唑并[2,1-b][1,3,4]噻二唑-5-基)亚甲基-1,3-噻唑烷二酮的合成、降血糖、降血脂和 PPARγ 激动剂活性。
Synthesis, hypoglycaemic, hypolipidemic and PPARγ agonist activities of 5-(2-Alkyl/aryl-6-Arylimidazo[2,1-b][1,3,4]thiadiazol-5-yl)methylene-1,3-thiazolidinediones.
机构信息
Department of Chemistry, Karnatak University, Dharwad, India.
出版信息
Chem Biol Drug Des. 2013 Aug;82(2):147-55. doi: 10.1111/cbdd.12140. Epub 2013 Jul 1.
A novel series of 5-(2-alkyl/aryl-6-arylimidazo[2,1-b][1,3,4]thiadiazol-5-yl)methylene-1,3-thiazolidinediones were synthesized as possible PPARγ agonists. The structures of these target molecules were established by spectral and analytical data. All the newly synthesized compounds were screened for their in vivo hypoglycaemic and hypolipidemic activity in male Wistar rats. Further, compounds with good activity were screened for PPARγ agonist activity. Among the screened compounds, 5-{[2-Cyclohexyl-6-(4-methoxyphenyl)imidazo[2,1-b] [1,3,4]thiadiazol-5-yl]methylene}-1,3-thiazolidine-2,4-dione (3i) exhibits promising hypoglycaemic and hypolipidemic activity via potential PPARγ agonist activity.
我们合成了一系列新型的 5-(2-烷基/芳基-6-芳基咪唑并[2,1-b][1,3,4]噻二唑-5-基)亚甲基-1,3-噻唑烷二酮作为潜在的 PPARγ 激动剂。这些目标分子的结构通过光谱和分析数据得到了确证。所有新合成的化合物都在雄性 Wistar 大鼠中进行了体内降血糖和降血脂活性的筛选。此外，还对具有良好活性的化合物进行了 PPARγ 激动剂活性的筛选。在所筛选的化合物中，5-[[2-环己基-6-(4-甲氧基苯基)咪唑并[2,1-b][1,3,4]噻二唑-5-基]亚甲基]-1,3-噻唑烷-2,4-二酮（3i）通过潜在的 PPARγ 激动剂活性表现出有前途的降血糖和降血脂活性。
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