| Synthesis and dual PPARalpha/delta agonist effects of 1,4-disubstituted 1,2,3-triazole analogues of GW 501516. | |
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MedLine Citation:
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PMID: 20403648 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Ten 1,4-disubstituted 1,2,3-triazoles 2a-2j were prepared and tested for their ability to increase oleic acid oxidation in human myotubes using a high-throughput multiwell assay. Compounds 2e (2-{4-[(1-(3-fluoro-4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) and 2i (2-{4-[(1-(3-chloro-4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) exhibited potent agonist activities. Compounds 2e and 2i also exhibited powerful agonist effects for both PPARalpha and PPARdelta in a luciferase-based assay. Consequently, these triazoles can be categorized as dual PPAR agonists. |
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Authors:
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Calin C Ciocoiu; Natasa Nikolić; Huyen Hoa Nguyen; G Hege Thoresen; Arne J Aasen; Trond Vidar Hansen |
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Publication Detail:
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Type: Journal Article Date: 2010-03-27 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 45 ISSN: 1768-3254 ISO Abbreviation: Eur J Med Chem Publication Date: 2010 Jul |
Date Detail:
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Created Date: 2010-05-17 Completed Date: 2010-08-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 3047-55 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010 Elsevier Masson SAS. All rights reserved. |
Affiliation:
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School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO BOX 1068, Blindern, N-0316 Oslo, Norway. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals COS Cells Cercopithecus aethiops Humans PPAR alpha / agonists* PPAR delta / agonists* Thiazoles / chemistry* Triazoles / chemical synthesis, chemistry*, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/GW 501516; 0/PPAR alpha; 0/PPAR delta; 0/Thiazoles; 0/Triazoles |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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