Novel phenoxyalkylcarboxylic acid derivatives as hypolipidaemic agents
Novel phenoxyalkyltcarboxylic acid derivatives based on the natural scaffolds,flavonoids,or resveratrol were designed,synthesized,and evaluated for hypolipidaemic activity.Among the compounds,30b lowered the triglycerides by 48.59% (P<0.05) and total cholesterol by 44.296 (P<0.05),respectively,and was more effective than the reference drug fenofibric acid in a Triton WR-1339-induced hyperlipidaemic mice model orally (300 mg/kg body weight).30b also showed 59.4% triglycerides lowering in an alloxan-induced diabetic mice model orally (150 mg/kg body weight).Receptor docking studies revealed that compound 30b could interact with the amino acid residues in the ligandbinding domain essential for the activation of the PPARα.The results indicate that resveratrol should be a better scaffold to derive a new class of hypolipidaemic agents in comparison with a flavonoid scaffold.
Scaffolds flavonoids resveratrol hypolipidaemic PPARα
Wei Li Hao-yan Jia Xin-hua He Wei-guo Shi Bo-hua Zhong
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicolagy, Beijing, P Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicolagy, Beijing, P
国际会议
南京
英文
392-399
2012-05-13（万方平台首次上网日期，不代表论文的发表时间）