3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 1230 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 3 N/A N/A Details