TY - JOUR
T1 - Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists
AU - Giampietro, Letizia
AU - Ammazzalorso, Alessandra
AU - Giancristofaro, Antonella
AU - Lannutti, Fabio
AU - Bettoni, Giancarlo
AU - De Filippis, Barbara
AU - Fantacuzzi, Marialuigia
AU - Maccallini, Cristina
AU - Petruzzelli, Michele
AU - Morgano, Annalisa
AU - Moschetta, Antonio
AU - Amoroso, Rosa
PY - 2009/10/22
Y1 - 2009/10/22
N2 - Aseries of 2-heteroarylthioalkanoic acids were synthesized through systematic structural modifications of clofibric acid and evaluated for human peroxisome proliferator-activated receptor α (PPARα) transactivation activity, with the aim of obtaining new hypolipidemic compounds. Some thiophene and benzothiazole derivatives showing a good activation of the receptor α were screened for activity against the PPARγ isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.
AB - Aseries of 2-heteroarylthioalkanoic acids were synthesized through systematic structural modifications of clofibric acid and evaluated for human peroxisome proliferator-activated receptor α (PPARα) transactivation activity, with the aim of obtaining new hypolipidemic compounds. Some thiophene and benzothiazole derivatives showing a good activation of the receptor α were screened for activity against the PPARγ isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.
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U2 - 10.1021/jm900878u
DO - 10.1021/jm900878u
M3 - Article
C2 - 19791744
AN - SCOPUS:70350061743
SN - 0022-2623
VL - 52
SP - 6224
EP - 6232
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 20
ER -