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    
Abstract/OtherAbstract:
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.
Authors:
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    
Affiliation:
Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy.
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MeSH Terms
Descriptor/Qualifier:
Cell Line, Tumor
Clofibric Acid / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology*
Humans
Oxygen / chemistry
PPAR alpha / agonists*,  genetics
Stereoisomerism
Sulfur / chemistry*
Transcriptional Activation
Grant Support
ID/Acronym/Agency:
GGP08259//Telethon
Chemical
Reg. No./Substance:
0/PPAR alpha; 7704-34-9/Sulfur; 7782-44-7/Oxygen; 882-09-7/Clofibric Acid

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


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