کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1359746 981412 2009 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
4-(3-Aryloxyaryl)quinoline alcohols are liver X receptor agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
4-(3-Aryloxyaryl)quinoline alcohols are liver X receptor agonists
چکیده انگلیسی

A series of 4-(3-aryloxyaryl)quinolines with alcohol substituents on the terminal aryl ring was prepared as potential LXR agonists, in which an alcohol group replaced an amide in previously reported amide analogs. High affinity LXR ligands with excellent agonist potency and efficacy in a functional model of LXR activity were identified, demonstrating that alcohols can substitute for amides while retaining LXR activity. The most potent compound was 5b which had an IC50 = 3.3 nM for LXRβ binding and EC50 = 12 nM (122% efficacy relative to T0901317) in an ABCA1 mRNA induction assay in J774 mouse cells.

A series of 4-(3-aryloxyaryl)quinolines 5 was prepared as LXR agonists.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 23, 1 December 2009, Pages 8086–8092
نویسندگان
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