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Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Aug2011, Vol. 21 Issue 16, p4869-4872. 4p. - Publication Year :
- 2011
-
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]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 21
- Issue :
- 16
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 63560948
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.06.028