Your browser doesn't support javascript.
loading
Novel phenoxyalkylcarboxylic acid derivatives as hypolipidaemic agents.
Li, Wei; Jia, Hao-yan; He, Xin-hua; Shi, Wei-guo; Zhong, Bo-hua.
Afiliação
  • Li W; Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing, P.R. China.
J Enzyme Inhib Med Chem ; 27(2): 311-8, 2012 Apr.
Article em En | MEDLINE | ID: mdl-22085137
Novel phenoxyalkylcarboxylic 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 48.5% (P < 0.05) and total cholesterol by 44.2% (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 ligand-binding 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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácidos Carboxílicos / Diabetes Mellitus Experimental / Hiperlipidemias / Hipolipemiantes Limite: Animals Idioma: En Ano de publicação: 2012 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácidos Carboxílicos / Diabetes Mellitus Experimental / Hiperlipidemias / Hipolipemiantes Limite: Animals Idioma: En Ano de publicação: 2012 Tipo de documento: Article