1. Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists
- Author
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Ammazzalorso, Alessandra, Giancristofaro, Antonella, D’Angelo, Alessandra, Filippis, Barbara De, Fantacuzzi, Marialuigia, Giampietro, Letizia, Maccallini, Cristina, and Amoroso, Rosa
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CHEMICAL inhibitors , *THIAZOLES , *AMIDES , *NUCLEAR receptors (Biochemistry) , *DRUG development , *ORGANIC synthesis , *THERAPEUTICS ,SULFONAMIDE drugs - Abstract
Abstract: The discovery of PPAR antagonists is emerging as an useful tool for elucidating the biological role of the receptor. Here we report the identification of N-(phenylsulfonyl)amides containing the benzothiazole scaffold, a novel class of potent PPARα antagonists obtained from chemical modification of carboxylic acid agonists. In this work, a group of phenylsulfonamides were synthesized and in vitro evaluated against the agonistic effect of GW7647; they showed an inhibitory effect on PPARα activation, with best compounds revealing a dose-dependent antagonistic profile. Some of these antagonists showed also an inhibitory effect on CPT1A pattern expression. [Copyright &y& Elsevier]
- Published
- 2011
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