Epple, Robert, Azimioara, Mihai, Russo, Ross, Bursulaya, Badry, Tian, Shin-Shay, Gerken, Andrea and Iskandar, Maya (2006) 1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists. Bioorganic & Medicinal Chemistry Letters, 16 (11). pp. 2969-2973. ISSN 0960-894X

Abstract

A series of highly potent and selective PPARdelta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 microM, making it a useful tool in studying the biological effects of selective PPARdelta activation.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Additional Information:	author can archive post-print (ie final draft post-refereeing)
Keywords:	Nuclear receptors; Peroxisome proliferator-activated receptor delta; PPAR agonists; Virtual docking
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Date Deposited:	14 Dec 2009 14:04
Last Modified:	31 Jan 2013 01:26
URI:	https://oak.novartis.com/id/eprint/153