| Literature DB >> 16931011 |
Robert Epple1, Mihai Azimioara, Ross Russo, Yongping Xie, Xing Wang, Christopher Cow, John Wityak, Don Karanewsky, Badry Bursulaya, Andreas Kreusch, Tove Tuntland, Andrea Gerken, Maya Iskandar, Enrique Saez, H Martin Seidel, Shin-Shay Tian.
Abstract
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.Entities:
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Year: 2006 PMID： 16931011 DOI： 10.1016/j.bmcl.2006.08.052
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823