3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists.: Part 2
3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists.: Part 2
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DOI：
10.1016/j.bmcl.2006.08.052
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发表时间：
2006-11-01
影响因子：
2.7
通讯作者：
Tian, Shin-Shay
中科院分区：
文献类型：
--
作者：
Epple, Robert;Azimioara, Mihai;Tian, Shin-Shay
A series of PPAR delta-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LC1765 (17d) was found to be a potent and selective PPAR delta agonist with good in vivo PK properties in mouse (C-max = 5.1 mu M, t(1/2) = 3.1 h). LC1765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LC1765 and the LBD of PPAR delta is discussed. (c) 2006 Elsevier Ltd. All rights reserved.
