Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists.

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 Lett

authors

Ammazzalorso A,Giancristofaro A,D'Angelo A,Filippis BD,Fantacuzzi M,Giampietro L,Maccallini C,Amoroso R

doi

10.1016/j.bmcl.2011.06.028

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4869-72

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00811-0

journal_volume

21

pub_type

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