| Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists. | |
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MedLine Citation:
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PMID: 19791744 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 52 ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2009 Oct |
Date Detail:
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Created Date: 2009-10-15 Completed Date: 2009-11-24 Revised Date: 2011-11-24 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 6224-32 Citation Subset: IM |
Affiliation:
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Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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GGP08259//Telethon |
| Chemical | |
Reg. No./Substance:
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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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