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

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


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
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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
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26


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