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

Epple, Robert and Russo, Ross and Azimioara, Mihai and Cow, Christopher and Xie, Yongping and Wang, Xing and Wityak, John and Karanewsky, Donald and Gerken, Andrea and Iskandar, Maya and Saez, Enrique and 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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