Author/Authors :
Robert Epple، نويسنده , , Ross Russo، نويسنده , , Mihai Azimioara، نويسنده , , Christopher Cow، نويسنده , , Yongping Xie، نويسنده , , Xing Wang، نويسنده , , John Wityak، نويسنده , , Don Karanewsky، نويسنده , , Andrea Gerken، نويسنده , , Maya Iskandar، نويسنده , , Enrique Saez، نويسنده , , H. Martin Seidel، نويسنده , , Shin-Shay Tian، نويسنده ,
Abstract :
We report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARδ. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.
Keywords :
PPAR? agonists , Energy homeostasis , isoxazoles , metabolic syndrome