کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360214 | 981428 | 2009 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Biarylether amide quinolines as liver X receptor agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 4-(amido-biarylether)-quinolines was prepared as potential LXR agonists. Appropriate substitution with amide groups provided high affinity LXR ligands, some with excellent potency and efficacy in functional assays of LXR activity. Novel amide 4g had a binding IC50 = 1.9 nM for LXRβ and EC50 = 34 nM (96% efficacy relative to T0901317) in an ABCA1 gene expression assay in mouse J774 cells, demonstrating that 4-(biarylether)-quinolines with appropriate amide substitution are potent LXR agonists
A series of biarylether amide quinolines (4) was prepared as LXR agonists.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 4, 15 February 2009, Pages 1663–1670
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 4, 15 February 2009, Pages 1663–1670
نویسندگان
Ronald C. Bernotas, Robert R. Singhaus, David H. Kaufman, John Ullrich, Horace Fletcher III, Elaine Quinet, Ponnal Nambi, Rayomand Unwalla, Anna Wilhelmsson, Annika Goos-Nilsson, Mathias Farnegardh, Jay Wrobel,