gw-7647 and benzothiazole

gw-7647 has been researched along with benzothiazole* in 1 studies

Other Studies

1 other study(ies) available for gw-7647 and benzothiazole

Article	Year
Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists. Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16 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. Topics: Benzothiazoles; Butyrates; Carnitine O-Palmitoyltransferase; Dose-Response Relationship, Drug; HEK293 Cells; Humans; Molecular Structure; Phenylurea Compounds; PPAR alpha; Stereoisomerism; Structure-Activity Relationship; Sulfonamides	2011

Article

Year

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

Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16

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.

Topics: Benzothiazoles; Butyrates; Carnitine O-Palmitoyltransferase; Dose-Response Relationship, Drug; HEK293 Cells; Humans; Molecular Structure; Phenylurea Compounds; PPAR alpha; Stereoisomerism; Structure-Activity Relationship; Sulfonamides

2011