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3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.

Epple, Robert, Azimioara, Mihai, Russo, Ross, Xie, Yongping, Wang, Xing, Cow, Christopher, Wityak, John, Karanewsky, Donald, Bursulaya, Badry, Kreusch, Andreas, Tuntland, Tove, Gerken, Andrea, Iskandar, Maya, Saez, Enrique, Seidel, Martin and Tian, Shin-Shay (2006) 3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2. Bioorganic & Medicinal Chemistry Letters, 16 (21). pp. 5488-5492. ISSN 0960-894X


A series of PPARdelta-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARdelta agonist with good in vivo PK properties in mouse (C(max)=5.1 microM, t(1/2)=3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARdelta is discussed.

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: Nuclear hormone receptor; PPAR agonist; PPARδ; Energy homeostasis; Metabolic xyndrome; Isoxazoles
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26


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