3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.

Article Details

Citation

Epple R, Russo R, Azimioara M, Cow C, Xie Y, Wang X, Wityak J, Karanewsky D, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS

3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4376-80. Epub 2006 Jun 5.

PubMed ID
16750626 [ View in PubMed
]
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 PPARdelta. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CardarinePeroxisome proliferator-activated receptor alphaEC 50 (nM)1230N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor deltaEC 50 (nM)3N/AN/ADetails