Document Detail


Novel phenoxyalkylcarboxylic acid derivatives as hypolipidaemic agents.
MedLine Citation:
PMID:  22085137     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Wei Li; Hao-yan Jia; Xin-hua He; Wei-guo Shi; Bo-hua Zhong
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Publication Detail:
Type:  Journal Article     Date:  2011-11-15
Journal Detail:
Title:  Journal of enzyme inhibition and medicinal chemistry     Volume:  27     ISSN:  1475-6374     ISO Abbreviation:  J Enzyme Inhib Med Chem     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-03-05     Completed Date:  2012-07-17     Revised Date:  2013-06-03    
Medline Journal Info:
Nlm Unique ID:  101150203     Medline TA:  J Enzyme Inhib Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  311-8     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing, P.R. China.
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MeSH Terms
Descriptor/Qualifier:
Animals
Carboxylic Acids / chemistry*
Cholesterol / metabolism
Diabetes Mellitus, Experimental / drug therapy*
Fenofibrate / analogs & derivatives,  toxicity
Flavonoids / chemistry
Hyperlipidemias / chemically induced,  drug therapy*
Hypolipidemic Agents / chemical synthesis*,  pharmacology*
Magnetic Resonance Spectroscopy
Male
Mice
Models, Molecular
Molecular Structure
Polyethylene Glycols / toxicity
Stilbenes / chemistry
Surface-Active Agents / toxicity
Triglycerides / metabolism
Chemical
Reg. No./Substance:
0/Carboxylic Acids; 0/Flavonoids; 0/Hypolipidemic Agents; 0/Polyethylene Glycols; 0/Stilbenes; 0/Surface-Active Agents; 0/Triglycerides; 25301-02-4/tyloxapol; 49562-28-9/Fenofibrate; 57-88-5/Cholesterol; BGF9MN2HU1/fenofibric acid; Q369O8926L/resveratrol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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