Epple, Robert, Russo, Ross, Azimioara, Mihai, Cow, Christopher, Xie, Yongping, Wang, Xing, Wityak, John, Karanewsky, Donald, Gerken, Andrea, Iskandar, Maya, Saez, Enrique, Seidel, Martin and Tian, Shin-Shay (2006) 3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1. Bioorganic & Medicinal Chemistry Letters, 16 (16). pp. 4376-4380. ISSN 0960-894X

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.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.05.055
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	PPARδ agonists; Metabolic syndrome; Energy homeostasis; Isoxazoles
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.05.055
Date Deposited:	14 Dec 2009 14:04
Last Modified:	31 Jan 2013 01:26
URI:	https://oak.novartis.com/id/eprint/148