Document Detail


Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
MedLine Citation:
PMID:  17157019     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to apply as PPARalpha and gamma dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in PPARalpha and gamma, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.
Authors:
Hee Oon Han; Seung Hae Kim; Kyoung-Hee Kim; Gwong-Cheung Hur; Hyeon Joo Yim; Hee-Kyung Chung; Sung Ho Woo; Ki Dong Koo; Chang-Seok Lee; Jong Sung Koh; Geun Tae Kim
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Publication Detail:
Type:  Journal Article     Date:  2006-11-18
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  17     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2007 Feb 
Date Detail:
Created Date:  2007-02-05     Completed Date:  2007-04-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  937-41     Citation Subset:  IM    
Affiliation:
Research and Development, LG Life Sciences, 104-1 Munji-dong, Yuseong-gu, Daejon 305-380, Republic of Korea.
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MeSH Terms
Descriptor/Qualifier:
Animals
Area Under Curve
Biological Availability
Blood Glucose / metabolism
Cell Line, Tumor
Drug Design
Humans
Hypoglycemic Agents / chemical synthesis*,  pharmacokinetics,  pharmacology*
Indicators and Reagents
Lipids / blood
Magnetic Resonance Spectroscopy
Mass Spectrometry
Mice
Models, Molecular
PPAR alpha / agonists*
PPAR gamma / agonists*
Phenylpropionates / chemical synthesis*,  pharmacology*
Structure-Activity Relationship
Thiazolidinediones / pharmacology
Triglycerides / blood
Chemical
Reg. No./Substance:
0/Blood Glucose; 0/Hypoglycemic Agents; 0/Indicators and Reagents; 0/Lipids; 0/PPAR alpha; 0/PPAR gamma; 0/Phenylpropionates; 0/Thiazolidinediones; 0/Triglycerides; 122320-73-4/rosiglitazone

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


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