Document Detail

Synthesis and dual PPARalpha/delta agonist effects of 1,4-disubstituted 1,2,3-triazole analogues of GW 501516.
MedLine Citation:
PMID:  20403648     Owner:  NLM     Status:  MEDLINE    
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.
Calin C Ciocoiu; Natasa Nikolić; Huyen Hoa Nguyen; G Hege Thoresen; Arne J Aasen; Trond Vidar Hansen
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Publication Detail:
Type:  Journal Article     Date:  2010-03-27
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  45     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-05-17     Completed Date:  2010-08-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  3047-55     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.
School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO BOX 1068, Blindern, N-0316 Oslo, Norway.
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MeSH Terms
COS Cells
Cercopithecus aethiops
PPAR alpha / agonists*
PPAR delta / agonists*
Thiazoles / chemistry*
Triazoles / chemical synthesis,  chemistry*,  pharmacology*
Reg. No./Substance:
0/GW 501516; 0/PPAR alpha; 0/PPAR delta; 0/Thiazoles; 0/Triazoles

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