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

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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

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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