کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376481 | 981959 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2 3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2](/preview/png/1376481.png)
چکیده انگلیسی
A series of PPARδ-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARδ agonist with good in vivo PK properties in mouse (Cmax = 5.1 μM, t1/2 = 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 PPARδ is discussed.
The optimization of an isoxazole series to the potent, selective, and bioavailable PPARδ agonist LCI765 is reported. A co-crystal structure and in vivo properties of LCI765 are discussed.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5488–5492
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5488–5492
نویسندگان
Robert Epple, 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,