| Novel phenoxyalkylcarboxylic acid derivatives as hypolipidaemic agents. | |
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MedLine Citation:
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PMID: 22085137 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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 PPAR?. The results indicate that resveratrol should be a better scaffold to derive a new class of hypolipidaemic agents in comparison with a flavonoid scaffold. |
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Authors:
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Wei Li; Hao-Yan Jia; Xin-Hua He; Wei-Guo Shi; Bo-Hua Zhong |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-11-15 |
Journal Detail:
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Title: Journal of enzyme inhibition and medicinal chemistry Volume: - ISSN: 1475-6374 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-11-16 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101150203 Medline TA: J Enzyme Inhib Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology , Beijing , P.R. China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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