Phenoxyacetic acids as PPARdelta partial agonists: synthesis, optimization, and in vivo efficacy.

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Evans KA, Shearer BG, Wisnoski DD, Shi D, Sparks SM, Sternbach DD, Winegar DA, Billin AN, Britt C, Way JM, Epperly AH, Leesnitzer LM, Merrihew RV, Xu RX, Lambert MH, Jin J

Phenoxyacetic acids as PPARdelta partial agonists: synthesis, optimization, and in vivo efficacy.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2345-50. doi: 10.1016/j.bmcl.2011.02.077. Epub 2011 Mar 15.

PubMed ID

21414782 [ View in PubMed

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Abstract

A series of phenoxyacetic acids as subtype selective and potent hPPARdelta partial agonists is described. Many analogues were readily accessible via a single solution-phase synthetic route which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of two potent exemplars which were further evaluated in vivo. Details of the SAR, optimization, and in vivo efficacy of this series are presented herein.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cardarine	Peroxisome proliferator-activated receptor alpha	IC 50 (nM)	1995.26	N/A	N/A	Details
Cardarine	Peroxisome proliferator-activated receptor delta	IC 50 (nM)	5.01	N/A	N/A	Details
Cardarine	Peroxisome proliferator-activated receptor delta	EC 50 (nM)	3.16	N/A	N/A	Details