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 PPARγ isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.
Synthesis and Biological Evaluation of 2-Heteroarylthioalkanoic Acid Analogues of Clofibric Acid as Peroxisome Proliferator-Activated Receptor alfa Agonists
GIAMPIETRO, Letizia;AMMAZZALORSO, Alessandra;GIANCRISTOFARO, ANTONELLA;LANNUTTI, FABIO;BETTONI, Giancarlo;DE FILIPPIS, Barbara;FANTACUZZI, MARIALUIGIA;MACCALLINI, Cristina;AMOROSO, Rosa
2009-01-01
Abstract
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 PPARγ isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.File in questo prodotto:
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