1区 · 医学
Article
作者: Amoroso, Rosa ; Giancristofaro, Antonella ; Ammazzalorso, Alessandra ; Moschetta, Antonio ; Giampietro, Letizia ; De Filippis, Barbara ; Maccallini, Cristina ; Petruzzelli, Michele ; Bettoni, Giancarlo ; Lannutti, Fabio ; Morgano, Annalisa ; Fantacuzzi, Marialuigia
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.