Microwave-Assisted Synthesis, Hypolipidemic and Hypoglycemic Activity of Some Novel 2-(4-(2-Amino-6-(4-substituted phenyl)-pyrimidin-4-yl)-phenoxy)-2-methyl Propanoic Acid Derivatives
作者:Santosh N. Mokale、Rupali D. Elgire、Nikhil S. Sakle、Devanand B. Shinde
DOI:10.1002/ardp.201000229
日期:2012.1
A novel series of aminopyrimidines containing the phenoxy isobutyric acid group as a pharmacophore was synthesized using conventional and microwave assisted methods of synthesis. The compounds were synthesized in good yields (70–89%) by the microwave‐assisted one‐pot protocol in much shorter reaction times. The synthesized compounds were evaluated for their hypolipidemic and hypoglycemic activity by
使用常规和微波辅助合成方法合成了一系列含有苯氧基异丁酸基团作为药效团的新型氨基嘧啶。通过微波辅助一锅法在更短的反应时间内以良好的收率(70-89%)合成了这些化合物。通过高脂肪饮食诱导的高脂血症和雄性 Sprague-Dawley 大鼠的高血糖来评估合成的化合物的降血脂和降血糖活性。本研究表明,与标准药物相比,该系列的所有化合物具有显着的抗高血脂和抗高血糖活性。该系列的构效关系 (SAR) 是通过比较合成化合物与作为标准药物的非诺贝特的总脂质谱数据而开发的。