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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Ammazzalorso A,Giancristofaro A,D'Angelo A,Filippis BD,Fantacuzzi M,Giampietro L,Maccallini C,Amoroso Rdoi
10.1016/j.bmcl.2011.06.028subject
Has Abstractpub_date
2011-08-15 00:00:00pages
4869-72issue
16eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)00811-0journal_volume
21pub_type
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