Molecular design, synthesis, and hypoglycemic and hypolipidemic activities of novel pyrimidine derivatives having thiazolidinedione

Molecular design, synthesis, and hypoglycemic and hypolipidemic activities of novel pyrimidine derivatives having thiazolidinedione
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DOI:
10.1016/j.ejmech.2005.03.019
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发表时间:
2005-09-01
影响因子:
6.7
通讯作者:
Yoon, SS
Yoon, SS
中科院分区:
医学1区
文献类型:
--
作者:
Lee, HW;Kim, BY;Yoon, SS

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我们以前报道了具有降血糖和降血脂活性的新型取代的含噻唑烷二酮的吡啶和嘌呤类化合物的合成和生物活性。本文报道了新型含噻唑烷二酮取代嘧啶类化合物的合成及其抗糖尿病活性。在KKA(y)小鼠中评价这些化合物(条目号5a-i、10a-d和16)的降葡萄糖和降脂质活性。结果表明,新化合物5c和5g分别比参比化合物吡格列酮和罗格列酮具有更强的生物活性。(c)2005年,Elsevier SAS。All rights reserved.
We previously reported the synthesis and biological activity of novel substituted pyridines and purines having thiazolidinedione with hypoglycemic and hypolipidemic activities. We now report the synthesis and antidiabetic activity of novel substituted pyrimidines having thiazolidinedione moiety. These compounds (entry No. 5a-i, 10a-d and 16) were evaluated for their glucose and lipid lowering activity in KKA(y) mice. From the results, novel compounds, 5c and 5g, exhibited considerably more potent biological activity than that of the reference compounds, pioglitazone and rosiglitazone, respectively. (c) 2005 Elsevier SAS. All rights reserved.