Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione
Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione
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DOI：
10.1016/j.ejmech.2004.03.001
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发表时间：
2004-05-01
影响因子：
6.7
通讯作者：
Yoon, SS
中科院分区：
文献类型：
--
作者：
Kim, BY;Ahn, JB;Yoon, SS
以相应的吡啶和嘌呤为原料，设计合成了一系列含有2,4-噻唑烷二酮的取代吡啶和嘌呤。这些合成化合物(条目号：6a-d、12a-e、18a-d、23a-c)在体外对3T3-L1细胞甘油三酯积累的影响，以及它们在体内对遗传性糖尿病KKA(y)小鼠的降糖和降血脂活性。根据其生物活性，选择5-（4-{2-[n-甲基-（5-苯基吡啶-2-基）氨基]乙氧基}苄基）噻唑烷-2,4-二酮（6d）作为进一步药理研究的候选物质。(C) 2004 Elsevier SAS。版权所有。
A series of substituted pyridines and purines containing 2,4-thiazolidinedione were designed and synthesized from their corresponding pyridines and purines. These synthesized compounds (entry no. 6a-d, 12a-e, 18a-d, 23a-c) were evaluated for their effect on triglyceride accumulation in 3T3-L1 cells in vitro and their hypoglycemic and hypolipidemic activity in the genetically diabetic KKA(y) mice in vivo. On the basis of their biological activities, 5-(4-{2-[N-methyl-(5-phenyl-pyridin-2-yl)amino]ethoxy}benzyl)thiazolidine-2,4-dione (6d) was selected as a candidate for further pharmacological studies. (C) 2004 Elsevier SAS. All rights reserved.