Synthesis and Biological Evaluation of tert‐Butyl‐5‐methylpyrimidin‐piperazine Derivatives as Anti‐Obesity Agents. Issue 12 (15th September 2014)

• Record Type: Journal Article
• Authors: Chen, Jinying; Pu, Yuzhi; Pei, Heying; He, Linhong; Fu, Suhong; Chen, Lijuan
• Is Part Of: Archiv der Pharmazie. Volume 347:Issue 12(2014:Dec.)
• Page Start: 908
• Page End: 922
• Publication Date: 2014-09-15
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201400227
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="ardp201400227-sec-0001" sec-type="section"> <p>A series of <italic>tert</italic>‐butyl‐5‐methylpyrimidin‐piperazine derivatives were synthesized and their anti‐obesity activities were evaluated. Compounds <bold>4g</bold> and <bold>5j</bold> were found to have significant effects in down‐regulating the triglyceride level of 3T3‐L1 adipocytes. <bold>5j</bold> exhibited remarkable therapeutic effects on the diet‐induced obesity (DIO) mouse model at 20 mg kg⁻¹ day⁻¹ for 4 weeks by decreasing the weights of body, liver, and fat. <bold>5j</bold> also regulated serum biomarkers to appropriate ranges, exerted therapeutic activity of steatosis in liver tissue and ameliorated the obese‐related symptoms. In addition, <bold>5j</bold> significantly decreased the blood glucose levels in oral glucose tolerance tests and improved the insulin sensitivity in insulin tolerance tests. These results suggest that <bold>5j</bold> could be a candidate for obesity treatment.</p> </sec> </abstract>