Novel glitazones: Design, synthesis, glucose uptake and structure-activity relationships

被引：42
|
作者：
Kumar, B. R. Prashantha [2 ]
Nanjan, M. J. [1 ]
机构：
[1] JSS Coll Pharm, TIFAC CORE, Ootacamund 643001, Tamil Nadu, India
[2] JSS Coll Pharm, Dept Pharmaceut Chem, Ootacamund 643001, Tamil Nadu, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 06期
关键词：
Glitazones; Glucose uptake; Diabetes; PPAR-gamma; Antidiabetic activity; PROLIFERATOR-ACTIVATED RECEPTORS; LIGANDS; AGENTS;
D O I：
10.1016/j.bmcl.2010.01.125
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1953 / 1956
页数：4
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