Document Detail

Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists.
MedLine Citation:
PMID:  19791744     Owner:  NLM     Status:  MEDLINE    
A series of 2-heteroarylthioalkanoic acids were synthesized through systematic structural modifications of clofibric acid and evaluated for human peroxisome proliferator-activated receptor alpha (PPARalpha) transactivation activity, with the aim of obtaining new hypolipidemic compounds. Some thiophene and benzothiazole derivatives showing a good activation of the receptor alpha were screened for activity against the PPARgamma isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.
Letizia Giampietro; Alessandra Ammazzalorso; Antonella Giancristofaro; Fabio Lannutti; Giancarlo Bettoni; Barbara De Filippis; Marialuigia Fantacuzzi; Cristina Maccallini; Michele Petruzzelli; Annalisa Morgano; Antonio Moschetta; Rosa Amoroso
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  52     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2009 Oct 
Date Detail:
Created Date:  2009-10-15     Completed Date:  2009-11-24     Revised Date:  2011-11-24    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  6224-32     Citation Subset:  IM    
Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy.
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MeSH Terms
Cell Line, Tumor
Clofibric Acid / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology*
Oxygen / chemistry
PPAR alpha / agonists*,  genetics
Sulfur / chemistry*
Transcriptional Activation
Grant Support
Reg. No./Substance:
0/PPAR alpha; 7704-34-9/Sulfur; 7782-44-7/Oxygen; 882-09-7/Clofibric Acid

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