کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364226 981532 2007 13 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators
چکیده انگلیسی

A series of phenyl acetic acid based quinolines was prepared as LXR modulators. An SAR study in which the C-3 and C-8 positions of the quinoline core were varied led to the identification of two potent LXR agonists 23 and 27. Both compounds displayed good binding affinity for LXRβ and LXRα, and increased expression of ABCA1 in THP-1 cells. These two compounds also had desirable pharmacokinetic profiles in mice and displayed in vivo efficacy in a 12-week Apo E knockout mouse lesion model.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 10, 15 May 2007, Pages 3321–3333
نویسندگان
, , , , , , , , , , , , , , , , ,